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William C. Groutas - Publications

Affiliations: 
Wichita State University, Wichita, KS, United States 
Area:
Biochemistry, Pharmaceutical Chemistry
Website:
https://www.wichita.edu/academics/fairmount_college_of_liberal_arts_and_sciences/chemistry/People/Groutas/main.php

115 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2024 Kim Y, Pool E, Kim E, Dampalla CS, Nguyen HN, Johnson DK, Lovell S, Groutas WC, Chang K-O. Potent small molecule inhibitors against the 3C protease of foot-and-mouth disease virus. Microbiology Spectrum. e0337223. PMID 38466127 DOI: 10.1128/spectrum.03372-23  0.479
2023 Li P, Kim Y, Dampalla CS, Nhat Nguyen H, Meyerholz DK, Johnson DK, Lovell S, Groutas WC, Perlman S, Chang K-O. Potent 3CLpro inhibitors effective against SARS-CoV-2 and MERS-CoV in animal models by therapeutic treatment. Mbio. e0287823. PMID 38126789 DOI: 10.1128/mbio.02878-23  0.416
2023 Dampalla CS, Miller MJ, Kim Y, Zabiegala A, Nguyen HN, Madden TK, Thurman HA, Machen AJ, Cooper A, Liu L, Battaile KP, Lovell S, Chang KO, Groutas WC. Structure-guided design of direct-acting antivirals that exploit the gem-dimethyl effect and potently inhibit 3CL proteases of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2) and middle east respiratory syndrome coronavirus (MERS-CoV). European Journal of Medicinal Chemistry. 254: 115376. PMID 37080108 DOI: 10.1016/j.ejmech.2023.115376  0.538
2022 Dampalla CS, Nguyen HN, Rathnayake AD, Kim Y, Perera KD, Madden TK, Thurman HA, Machen AJ, Kashipathy MM, Liu L, Battaile KP, Lovell S, Chang KO, Groutas WC. Broad-Spectrum Cyclopropane-Based Inhibitors of Coronavirus 3C-like Proteases: Biochemical, Structural, and Virological Studies. Acs Pharmacology & Translational Science. 6: 181-194. PMID 36654747 DOI: 10.1021/acsptsci.2c00206  0.831
2022 Perera KD, Johnson D, Lovell S, Groutas WC, Chang KO, Kim Y. Potent Protease Inhibitors of Highly Pathogenic Lagoviruses: Rabbit Hemorrhagic Disease Virus and European Brown Hare Syndrome Virus. Microbiology Spectrum. e0014222. PMID 35766511 DOI: 10.1128/spectrum.00142-22  0.476
2022 Dampalla CS, Rathnayake AD, Galasiti Kankanamalage AC, Kim Y, Perera KD, Nguyen HN, Miller MJ, Madden TK, Picard HR, Thurman HA, Kashipathy MM, Liu L, Battaile KP, Lovell S, Chang KO, ... Groutas WC, et al. Structure-Guided Design of Potent Spirocyclic Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3C-like Protease. Journal of Medicinal Chemistry. 65: 7818-7832. PMID 35638577 DOI: 10.1021/acs.jmedchem.2c00224  0.832
2021 Dampalla CS, Rathnayake AD, Perera KD, Jesri AM, Nguyen HN, Miller MJ, Thurman HA, Zheng J, Kashipathy MM, Battaile KP, Lovell S, Perlman S, Kim Y, Groutas WC, Chang KO. Structure-Guided Design of Potent Inhibitors of SARS-CoV-2 3CL Protease: Structural, Biochemical, and Cell-Based Studies. Journal of Medicinal Chemistry. PMID 34865476 DOI: 10.1021/acs.jmedchem.1c01037  0.836
2021 Dampalla CS, Kim Y, Bickmeier N, Rathnayake AD, Nguyen HN, Zheng J, Kashipathy MM, Baird MA, Battaile KP, Lovell S, Perlman S, Chang KO, Groutas WC. Structure-Guided Design of Conformationally Constrained Cyclohexane Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3CL Protease. Journal of Medicinal Chemistry. PMID 34213885 DOI: 10.1021/acs.jmedchem.1c00319  0.826
2021 Dampalla CS, Zheng J, Perera KD, Wong LR, Meyerholz DK, Nguyen HN, Kashipathy MM, Battaile KP, Lovell S, Kim Y, Perlman S, Groutas WC, Chang KO. Postinfection treatment with a protease inhibitor increases survival of mice with a fatal SARS-CoV-2 infection. Proceedings of the National Academy of Sciences of the United States of America. 118. PMID 34210738 DOI: 10.1073/pnas.2101555118  0.364
2020 Rathnayake AD, Kim Y, Dampalla CS, Nguyen HN, Jesri AM, Kashipathy MM, Lushington GH, Battaile KP, Lovell S, Chang KO, Groutas WC. Structure-Guided Optimization of Dipeptidyl Inhibitors of Norovirus 3CL Protease. Journal of Medicinal Chemistry. PMID 32945669 DOI: 10.1021/Acs.Jmedchem.0C01252  0.845
2020 Rathnayake AD, Zheng J, Kim Y, Perera KD, Mackin S, Meyerholz DK, Kashipathy MM, Battaile KP, Lovell S, Perlman S, Groutas WC, Chang KO. 3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice. Science Translational Medicine. PMID 32747425 DOI: 10.1126/Scitranslmed.Abc5332  0.83
2019 Perera KD, Rathnayake AD, Liu H, Pedersen NC, Groutas WC, Chang KO, Kim Y. Characterization of amino acid substitutions in feline coronavirus 3C-like protease from a cat with feline infectious peritonitis treated with a protease inhibitor. Veterinary Microbiology. 237: 108398. PMID 31585653 DOI: 10.1016/J.Vetmic.2019.108398  0.787
2019 Galasiti Kankanamalage AC, Weerawarna PM, Rathnayake AD, Kim Y, Mehzabeen N, Battaile KP, Lovell S, Chang KO, Groutas WC. Putative Structural Rearrangements Associated with the Interaction of Macrocyclic Inhibitors with Norovirus 3CL Protease. Proteins. PMID 30883881 DOI: 10.1002/Prot.25682  0.833
2019 Chang KO, Kim Y, Lovell S, Rathnayake AD, Groutas WC. Antiviral Drug Discovery: Norovirus Proteases and Development of Inhibitors. Viruses. 11. PMID 30823509 DOI: 10.3390/V11020197  0.849
2018 Perera KD, Galasiti Kankanamalage AC, Rathnayake AD, Honeyfield A, Groutas W, Chang KO, Kim Y. Protease inhibitors broadly effective against feline, ferret and mink coronaviruses. Antiviral Research. PMID 30342822 DOI: 10.1016/J.Antiviral.2018.10.015  0.831
2018 Galasiti Kankanamalage AC, Kim Y, Damalanka VC, Rathnayake AD, Fehr AR, Mehzabeen N, Battaile KP, Lovell S, Lushington GH, Perlman S, Chang KO, Groutas WC. Structure-guided design of potent and permeable inhibitors of MERS coronavirus 3CL protease that utilize a piperidine moiety as a novel design element. European Journal of Medicinal Chemistry. 150: 334-346. PMID 29544147 DOI: 10.1016/J.Ejmech.2018.03.004  0.839
2018 Damalanka VC, Kim Y, Galasiti Kankanamalage AC, Rathnayake AD, Mehzabeen N, Battaile KP, Lovell S, Nguyen HN, Lushington GH, Chang KO, Groutas WC. Structure-guided design, synthesis and evaluation of oxazolidinone-based inhibitors of norovirus 3CL protease. European Journal of Medicinal Chemistry. 143: 881-890. PMID 29227928 DOI: 10.1016/J.Ejmech.2017.12.014  0.84
2017 Sun N, Li D, Zhang Y, Killeen K, Groutas W, Calderone R. Repurposing an inhibitor of ribosomal biogenesis with broad anti-fungal activity. Scientific Reports. 7: 17014. PMID 29209049 DOI: 10.1038/S41598-017-17147-X  0.453
2017 Pedersen NC, Kim Y, Liu H, Galasiti Kankanamalage AC, Eckstrand C, Groutas WC, Bannasch M, Meadows JM, Chang KO. Efficacy of a 3C-like protease inhibitor in treating various forms of acquired feline infectious peritonitis. Journal of Feline Medicine and Surgery. 1098612X17729626. PMID 28901812 DOI: 10.1177/1098612X17729626  0.587
2017 Galasiti Kankanamalage AC, Kim Y, Rathnayake AD, Alliston KR, Butler MM, Cardinale SC, Bowlin TL, Groutas WC, Chang KO. Design, Synthesis, and Evaluation of Novel Prodrugs of Transition State Inhibitors of Norovirus 3CL Protease. Journal of Medicinal Chemistry. PMID 28671827 DOI: 10.1021/Acs.Jmedchem.7B00497  0.826
2016 Damalanka VC, Kim Y, Galasiti Kankanamalage AC, Lushington GH, Mehzabeen N, Battaile KP, Lovell S, Chang KO, Groutas WC. Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease. European Journal of Medicinal Chemistry. 127: 41-61. PMID 28038326 DOI: 10.1016/J.Ejmech.2016.12.033  0.777
2016 Galasiti Kankanamalage AC, Kim Y, Rathnayake AD, Damalanka VC, Weerawarna PM, Doyle ST, Alsoudi AF, Dissanayake DM, Lushington GH, Mehzabeen N, Battaile KP, Lovell S, Chang KO, Groutas WC. Structure-based exploration and exploitation of the S4 subsite of norovirus 3CL protease in the design of potent and permeable inhibitors. European Journal of Medicinal Chemistry. 126: 502-516. PMID 27914364 DOI: 10.1016/J.Ejmech.2016.11.027  0.823
2016 Weerawarna PM, Kim Y, Galasiti Kankanamalage AC, Damalanka VC, Lushington GH, Alliston KR, Mehzabeen N, Battaile KP, Lovell S, Chang KO, Groutas WC. Structure-based design and synthesis of triazole-based macrocyclic inhibitors of norovirus protease: Structural, biochemical, spectroscopic, and antiviral studies. European Journal of Medicinal Chemistry. 119: 300-318. PMID 27235842 DOI: 10.1016/J.Ejmech.2016.04.013  0.849
2016 Kim Y, Liu H, Kankanamalage AC, Weerasekara S, Hua DH, Groutas WC, Chang KO, Pedersen NC. Correction: Reversal of the Progression of Fatal Coronavirus Infection in Cats by a Broad-Spectrum Coronavirus Protease Inhibitor. Plos Pathogens. 12: e1005650. PMID 27166862 DOI: 10.1371/Journal.Ppat.1005650  0.65
2016 Kim Y, Liu H, Galasiti Kankanamalage AC, Weerasekara S, Hua DH, Groutas WC, Chang KO, Pedersen NC. Reversal of the Progression of Fatal Coronavirus Infection in Cats by a Broad-Spectrum Coronavirus Protease Inhibitor. Plos Pathogens. 12: e1005531. PMID 27027316 DOI: 10.1371/Journal.Ppat.1005531  0.695
2016 Galasiti Kankanamalage AC, Weerawarna PM, Kim Y, Chang KO, Groutas WC. Anti-Norovirus Therapeutics: A Patent Review (2010-2015). Expert Opinion On Therapeutic Patents. PMID 26881878 DOI: 10.1517/13543776.2016.1153065  0.796
2016 Damalanka VC, Kim Y, Alliston KR, Weerawarna PM, Galasiti Kankanamalage AC, Lushington GH, Mehzabeen N, Battaile KP, Lovell SW, Chang KO, Groutas WC. Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease. Journal of Medicinal Chemistry. PMID 26823007 DOI: 10.1021/Acs.Jmedchem.5B01464  0.843
2015 Kim Y, Galasiti Kankanamalage AC, Damalanka VC, Weerawarna PM, Groutas WC, Chang KO. Potent Inhibition of Enterovirus D68 and Human Rhinoviruses by Dipeptidyl Aldehydes and α-Ketoamides. Antiviral Research. PMID 26658373 DOI: 10.1016/J.Antiviral.2015.11.010  0.796
2015 Kim Y, Galasiti Kankanamalage AC, Chang KO, Groutas WC. Recent Advances in the Discovery of Norovirus Therapeutics. Journal of Medicinal Chemistry. PMID 26258852 DOI: 10.1021/Acs.Jmedchem.5B00762  0.666
2015 Galasiti Kankanamalage AC, Kim Y, Weerawarna PM, Uy RA, Damalanka VC, Mandadapu SR, Alliston KR, Mehzabeen N, Battaile KP, Lovell S, Chang KO, Groutas WC. Structure-guided design and optimization of dipeptidyl inhibitors of norovirus 3CL protease. Structure-activity relationships and biochemical, X-ray crystallographic, cell-based, and in vivo studies. Journal of Medicinal Chemistry. 58: 3144-55. PMID 25761614 DOI: 10.1021/Jm5019934  0.839
2015 Kim Y, Shivanna V, Narayanan S, Prior AM, Weerasekara S, Hua DH, Kankanamalage AC, Groutas WC, Chang KO. Broad-spectrum inhibitors against 3C-like proteases of feline coronaviruses and feline caliciviruses. Journal of Virology. 89: 4942-50. PMID 25694593 DOI: 10.1128/Jvi.03688-14  0.749
2014 Calderone R, Sun N, Gay-Andrieu F, Groutas W, Weerawarna P, Prasad S, Alex D, Li D. Antifungal drug discovery: the process and outcomes. Future Microbiology. 9: 791-805. PMID 25046525 DOI: 10.2217/Fmb.14.32  0.783
2013 Prior AM, Kim Y, Weerasekara S, Moroze M, Alliston KR, Uy RA, Groutas WC, Chang KO, Hua DH. Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors. Bioorganic & Medicinal Chemistry Letters. 23: 6317-20. PMID 24125888 DOI: 10.1016/J.Bmcl.2013.09.070  0.688
2013 Takahashi D, Kim Y, Lovell S, Prakash O, Groutas WC, Chang KO. Structural and inhibitor studies of norovirus 3C-like proteases. Virus Research. 178: 437-44. PMID 24055466 DOI: 10.1016/J.Virusres.2013.09.008  0.692
2013 Mandadapu SR, Gunnam MR, Galasiti Kankanamalage AC, Uy RA, Alliston KR, Lushington GH, Kim Y, Chang KO, Groutas WC. Potent inhibition of norovirus by dipeptidyl α-hydroxyphosphonate transition state mimics. Bioorganic & Medicinal Chemistry Letters. 23: 5941-4. PMID 24054123 DOI: 10.1016/J.Bmcl.2013.08.073  0.671
2013 Mandadapu SR, Weerawarna PM, Prior AM, Uy RA, Aravapalli S, Alliston KR, Lushington GH, Kim Y, Hua DH, Chang KO, Groutas WC. Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus. Bioorganic & Medicinal Chemistry Letters. 23: 3709-12. PMID 23727045 DOI: 10.1016/J.Bmcl.2013.05.021  0.802
2013 Kim Y, Mandadapu SR, Groutas WC, Chang KO. Potent inhibition of feline coronaviruses with peptidyl compounds targeting coronavirus 3C-like protease. Antiviral Research. 97: 161-8. PMID 23219425 DOI: 10.1016/J.Antiviral.2012.11.005  0.753
2013 Mandadapu SR, Gunnam MR, Tiew KC, Uy RA, Prior AM, Alliston KR, Hua DH, Kim Y, Chang KO, Groutas WC. Inhibition of norovirus 3CL protease by bisulfite adducts of transition state inhibitors. Bioorganic & Medicinal Chemistry Letters. 23: 62-5. PMID 23218713 DOI: 10.1016/J.Bmcl.2012.11.026  0.702
2013 Lai H, Dou D, Aravapalli S, Teramoto T, Lushington GH, Mwania TM, Alliston KR, Eichhorn DM, Padmanabhan R, Groutas WC. Design, synthesis and characterization of novel 1,2-benzisothiazol-3(2H)-one and 1,3,4-oxadiazole hybrid derivatives: potent inhibitors of Dengue and West Nile virus NS2B/NS3 proteases. Bioorganic & Medicinal Chemistry. 21: 102-13. PMID 23211969 DOI: 10.1016/J.Bmc.2012.10.058  0.492
2012 Kim Y, Lovell S, Tiew KC, Mandadapu SR, Alliston KR, Battaile KP, Groutas WC, Chang KO. Broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, noroviruses, and coronaviruses. Journal of Virology. 86: 11754-62. PMID 22915796 DOI: 10.1128/Jvi.01348-12  0.735
2012 Mandadapu SR, Weerawarna PM, Gunnam MR, Alliston KR, Lushington GH, Kim Y, Chang KO, Groutas WC. Potent inhibition of norovirus 3CL protease by peptidyl α-ketoamides and α-ketoheterocycles. Bioorganic & Medicinal Chemistry Letters. 22: 4820-6. PMID 22698498 DOI: 10.1016/J.Bmcl.2012.05.055  0.808
2012 Aravapalli S, Lai H, Teramoto T, Alliston KR, Lushington GH, Ferguson EL, Padmanabhan R, Groutas WC. Inhibitors of Dengue virus and West Nile virus proteases based on the aminobenzamide scaffold. Bioorganic & Medicinal Chemistry. 20: 4140-8. PMID 22632792 DOI: 10.1016/J.Bmc.2012.04.055  0.538
2012 Dou D, Tiew KC, Mandadapu SR, Gunnam MR, Alliston KR, Kim Y, Chang KO, Groutas WC. Potent norovirus inhibitors based on the acyclic sulfamide scaffold. Bioorganic & Medicinal Chemistry. 20: 2111-8. PMID 22356738 DOI: 10.1016/J.Bmc.2012.01.030  0.731
2012 Tiew KC, Dou D, Teramoto T, Lai H, Alliston KR, Lushington GH, Padmanabhan R, Groutas WC. Inhibition of Dengue virus and West Nile virus proteases by click chemistry-derived benz[d]isothiazol-3(2H)-one derivatives. Bioorganic & Medicinal Chemistry. 20: 1213-21. PMID 22249124 DOI: 10.1016/J.Bmc.2011.12.047  0.433
2012 Dou D, He G, Mandadapu SR, Aravapalli S, Kim Y, Chang KO, Groutas WC. Inhibition of noroviruses by piperazine derivatives. Bioorganic & Medicinal Chemistry Letters. 22: 377-9. PMID 22119464 DOI: 10.1016/J.Bmcl.2011.10.122  0.679
2012 Dou D, Mandadapu SR, Alliston KR, Kim Y, Chang KO, Groutas WC. Cyclosulfamide-based derivatives as inhibitors of noroviruses. European Journal of Medicinal Chemistry. 47: 59-64. PMID 22063754 DOI: 10.1016/J.Ejmech.2011.10.019  0.715
2011 Dou D, Tiew KC, He G, Mandadapu SR, Aravapalli S, Alliston KR, Kim Y, Chang KO, Groutas WC. Potent inhibition of Norwalk virus by cyclic sulfamide derivatives. Bioorganic & Medicinal Chemistry. 19: 5975-83. PMID 21925886 DOI: 10.1016/J.Bmc.2011.08.054  0.682
2011 Dou D, Alex D, Du B, Tiew KC, Aravapalli S, Mandadapu SR, Calderone R, Groutas WC. Antifungal activity of a series of 1,2-benzisothiazol-3(2H)-one derivatives. Bioorganic & Medicinal Chemistry. 19: 5782-7. PMID 21903403 DOI: 10.1016/J.Bmc.2011.08.029  0.361
2011 Dou D, Mandadapu SR, Alliston KR, Kim Y, Chang KO, Groutas WC. Design and synthesis of inhibitors of noroviruses by scaffold hopping. Bioorganic & Medicinal Chemistry. 19: 5749-55. PMID 21893416 DOI: 10.1016/J.Bmc.2011.08.032  0.707
2011 Tiew KC, He G, Aravapalli S, Mandadapu SR, Gunnam MR, Alliston KR, Lushington GH, Kim Y, Chang KO, Groutas WC. Design, synthesis, and evaluation of inhibitors of Norwalk virus 3C protease. Bioorganic & Medicinal Chemistry Letters. 21: 5315-9. PMID 21802286 DOI: 10.1016/J.Bmcl.2011.07.016  0.752
2011 Dou D, He G, Alliston KR, Groutas WC. Dual function inhibitors of relevance to chronic obstructive pulmonary disease. Bioorganic & Medicinal Chemistry Letters. 21: 3177-80. PMID 21511470 DOI: 10.1016/J.Bmcl.2010.12.033  0.406
2011 Groutas WC, Dou D, Alliston KR. Neutrophil elastase inhibitors. Expert Opinion On Therapeutic Patents. 21: 339-54. PMID 21235378 DOI: 10.1517/13543776.2011.551115  0.342
2010 Dou D, Viwanathan P, Li Y, He G, Alliston KR, Lushington GH, Brown-Clay JD, Padmanabhan R, Groutas WC. Design, synthesis, and in vitro evaluation of potential West Nile virus protease inhibitors based on the 1-oxo-1,2,3,4-tetrahydroisoquinoline and 1-oxo-1,2-dihydroisoquinoline scaffolds. Journal of Combinatorial Chemistry. 12: 836-43. PMID 20882963 DOI: 10.1021/Cc100091H  0.542
2010 Dou D, He G, Kuang R, Fu Q, Venkataraman R, Groutas WC. Effects of structure on inhibitory activity in a series of mechanism-based inhibitors of human neutrophil elastase. Bioorganic & Medicinal Chemistry. 18: 6646-50. PMID 20728366 DOI: 10.1016/J.Bmc.2010.07.071  0.566
2010 He G, Dou D, Wei L, Alliston KR, Groutas WC. Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold. European Journal of Medicinal Chemistry. 45: 4280-7. PMID 20638756 DOI: 10.1016/J.Ejmech.2010.06.028  0.45
2010 Dou D, He G, Li Y, Lai Z, Wei L, Alliston KR, Lushington GH, Eichhorn DM, Groutas WC. Utilization of the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide scaffold in the design of potential inhibitors of human neutrophil proteinase 3. Bioorganic & Medicinal Chemistry. 18: 1093-102. PMID 20061159 DOI: 10.1016/J.Bmc.2009.12.057  0.471
2010 KUANG R, VENKATARAMAN R, RUAN S, GROUTAS WC. ChemInform Abstract: Use of the 1,2,5-Thiadiazolidin-3-one 1,1 Dioxide and Isothiazolidin-3-one 1,1 Dioxide Scaffolds in the Design of Potent Inhibitors of Serine Proteinases. Cheminform. 29: no-no. DOI: 10.1002/CHIN.199824120  0.33
2009 Li Y, Dou D, He G, Lushington GH, Groutas WC. Mechanism-based inhibitors of serine proteases with high selectivity through optimization of S' subsite binding. Bioorganic & Medicinal Chemistry. 17: 3536-42. PMID 19394830 DOI: 10.1016/J.Bmc.2009.04.011  0.531
2008 Yang Q, Li Y, Dou D, Gan X, Mohan S, Groutas CS, Stevenson LE, Lai Z, Alliston KR, Zhong J, Williams TD, Groutas WC. Inhibition of serine proteases by a new class of cyclosulfamide-based carbamylating agents. Archives of Biochemistry and Biophysics. 475: 115-20. PMID 18457652 DOI: 10.1016/J.Abb.2008.04.020  0.496
2008 Huang W, Yamamoto Y, Li Y, Dou D, Alliston KR, Hanzlik RP, Williams TD, Groutas WC. X-ray snapshot of the mechanism of inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives. Journal of Medicinal Chemistry. 51: 2003-8. PMID 18318470 DOI: 10.1021/Jm700966P  0.442
2008 Li Y, Yang Q, Dou D, Alliston KR, Groutas WC. Inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1 dioxide-based sulfonamides. Bioorganic & Medicinal Chemistry. 16: 692-8. PMID 17976994 DOI: 10.1016/J.Bmc.2007.10.041  0.481
2005 Wong T, Groutas CS, Mohan S, Lai Z, Alliston KR, Vu N, Schechter NM, Groutas WC. 1,2,5-Thiadiazolidin-3-one 1,1-dioxide-based heterocyclic sulfides are potent inhibitors of human tryptase. Archives of Biochemistry and Biophysics. 436: 1-7. PMID 15752703 DOI: 10.1016/J.Abb.2005.01.022  0.557
2004 Zhong J, Lai Z, Groutas CS, Wong T, Gan X, Alliston KR, Eichhorn D, Hoidal JR, Groutas WC. Serendipitous discovery of an unexpected rearrangement leads to two new classes of potential protease inhibitors. Bioorganic & Medicinal Chemistry. 12: 6249-54. PMID 15519167 DOI: 10.1016/J.Bmc.2004.08.044  0.531
2004 Zhong J, Groutas WC. Recent developments in the design of mechanism-based and alternate substrate inhibitors of serine proteases. Current Topics in Medicinal Chemistry. 4: 1203-16. PMID 15320721  0.43
2004 Lai Z, Gan X, Wei L, Alliston KR, Yu H, Li YH, Groutas WC. Potent inhibition of human leukocyte elastase by 1,2,5-thiadiazolidin-3-one 1,1 dioxide-based sulfonamide derivatives. Archives of Biochemistry and Biophysics. 429: 191-7. PMID 15313222 DOI: 10.1016/J.Abb.2004.06.014  0.55
2004 Wei L, Lai Z, Gan X, Alliston KR, Zhong J, Epp JB, Tu J, Perera AB, Van Stipdonk M, Groutas WC. Mechanism-based inactivation of human leukocyte elastase via an enzyme-induced sulfonamide fragmentation process. Archives of Biochemistry and Biophysics. 429: 60-70. PMID 15288810 DOI: 10.1016/J.Abb.2004.05.018  0.51
2004 Zhong J, Gan X, Alliston KR, Lai Z, Yu H, Groutas CS, Wong T, Groutas WC. Potential protease inhibitors based on a functionalized cyclic sulfamide scaffold. Journal of Combinatorial Chemistry. 6: 556-63. PMID 15244417 DOI: 10.1021/Cc030047R  0.522
2004 Zhong J, Gan X, Alliston KR, Groutas WC. Design, synthesis, and in vitro evaluation of inhibitors of human leukocyte elastase based on a functionalized cyclic sulfamide scaffold. Bioorganic & Medicinal Chemistry. 12: 589-93. PMID 14738969  0.464
2003 Wei L, Gan X, Zhong J, Alliston KR, Groutas WC. Noncovalent inhibitors of human leukocyte elastase based on the 4-imidazolidinone scaffold. Bioorganic & Medicinal Chemistry. 11: 5149-53. PMID 14604678  0.374
2001 Groutas WC, He S, Kuang R, Ruan S, Tu J, Chan HK. Inhibition of serine proteases by functionalized sulfonamides coupled to the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold. Bioorganic & Medicinal Chemistry. 9: 1543-8. PMID 11408173 DOI: 10.1016/S0968-0896(01)00037-2  0.636
2001 Groutas WC, Epp JB, Kuang R, Ruan S, Chong LS, Venkataraman R, Tu J, He S, Yu H, Fu Q, Li YH, Truong TM, Vu NT. 1,2,5-Thiadiazolidin-3-one 1,1 dioxide: a powerful scaffold for probing the S' subsites of (chymo)trypsin-like serine proteases. Archives of Biochemistry and Biophysics. 385: 162-9. PMID 11361013 DOI: 10.1006/Abbi.2000.2139  0.678
2001 He S, Yu H, Fu Q, Kuang R, Epp JB, Groutas WC. A one-step protocol for the N-chloromethylation of heterocyclic imides Synthetic Communications. 31: 3055-3058. DOI: 10.1081/Scc-100105876  0.476
2000 He S, Kuang R, Venkataraman R, Tu J, Truong TM, Chan HK, Groutas WC. Potent inhibition of serine proteases by heterocyclic sulfide derivatives of 1,2,5-thiadiazolidin-3-one 1,1 dioxide. Bioorganic & Medicinal Chemistry. 8: 1713-7. PMID 10976518 DOI: 10.1016/S0968-0896(00)00101-2  0.668
2000 Kuang R, Epp JB, Ruan S, Chong LS, Venkataraman R, Tu J, He S, Truong TM, Groutas WC. Utilization of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold in the design of potent inhibitors of serine proteases: SAR studies using carboxylates. Bioorganic & Medicinal Chemistry. 8: 1005-16. PMID 10882012 DOI: 10.1016/S0968-0896(00)00038-9  0.67
1999 Groutas WC, Schechter NM, He S, Yu H, Huang P, Tu J. Human chymase inhibitors based on the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold. Bioorganic & Medicinal Chemistry Letters. 9: 2199-204. PMID 10465545 DOI: 10.1016/S0960-894X(99)00377-7  0.675
1999 Kuang R, Epp JB, Ruan S, Yu H, Huang P, He S, Tu J, Schechter NM, Turbov J, Froelich CJ, Groutas WC. A General Inhibitor Scaffold for Serine Proteases with a (Chymo)trypsin-Like Fold:  Solution-Phase Construction and Evaluation of the First Series of Libraries of Mechanism-Based Inhibitors Journal of the American Chemical Society. 121: 8128-8129. DOI: 10.1021/Ja990160E  0.656
1998 Kuang R, Venkataraman R, Ruan S, Groutas WC. Use of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide and isothiazolidin-3-one 1,1 dioxide scaffolds in the design of potent inhibitors of serine proteinases Bioorganic and Medicinal Chemistry Letters. 8: 539-544. PMID 9871614 DOI: 10.1016/S0960-894X(98)00067-5  0.36
1998 Groutas WC, Kuang R, Ruan S, Epp JB, Venkataraman R, Truong TM. Potent and specific inhibition of human leukocyte elastase, cathepsin G and proteinase 3 by sulfone derivatives employing the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold. Bioorganic & Medicinal Chemistry. 6: 661-71. PMID 9681132 DOI: 10.1016/S0968-0896(98)00006-6  0.415
1997 Groutas WC, Ruan S, Kuang R, Hook JB, Sands H. Inhibition of human leukocyte proteinase 3 by a novel recombinant serine proteinase inhibitor (LEX032) Biochemical and Biophysical Research Communications. 233: 697-699. PMID 9168917 DOI: 10.1006/Bbrc.1997.6526  0.478
1997 Groutas WC, Kuang R, Venkataraman R, Epp JB, Ruan S, Prakash O. Structure-based design of a general class of mechanism-based inhibitors of the serine proteinases employing a novel amino acid-derived heterocyclic scaffold. Biochemistry. 36: 4739-50. PMID 9125494 DOI: 10.1021/Bi9628937  0.527
1997 Randall JC, Ambroso JL, Groutas WC, Brubaker MJ, Richardson RJ. Inhibition of neurotoxic esterase in vitro by novel carbamates Toxicology and Applied Pharmacology. 143: 173-178. PMID 9073605 DOI: 10.1006/Taap.1996.8082  0.395
1996 Groutas WC, Chong LS, Venkataraman R, Kuang R, Epp JB, Houser-Archield N, Huang H, Hoidal JR. Amino acid-derived phthalimide and saccharin derivatives as inhibitors of human leukocyte elastase, cathepsin G, and proteinase 3. Archives of Biochemistry and Biophysics. 332: 335-40. PMID 8806743 DOI: 10.1006/Abbi.1996.0350  0.401
1995 Groutas WC, Brubaker MJ, Chong LS, Venkataraman R, Huang H, Epp JB, Kuang R, Hoidal JR. Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3. Bioorganic & Medicinal Chemistry. 3: 375-81. PMID 8581420 DOI: 10.1016/0968-0896(95)00024-B  0.336
1995 Groutas WC, Huang H, Epp JB, Venkataraman R, McClenahan JJ, Tagusagawa F. Mechanism-based inhibition of human leukocyte elastase and cathepsin G by substituted dihydrouracils. Biochimica Et Biophysica Acta. 1227: 130-6. PMID 7986820 DOI: 10.1016/0925-4439(94)90087-6  0.477
1995 Groutas WC, Chong LS, Venkataraman R, Epp JB, Kuang R, Houser-Archield N, Hoidal JR. The Gabriel-Colman rearrangement in biological systems: design, synthesis and biological evaluation of phthalimide and saccharin derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3. Bioorganic & Medicinal Chemistry. 3: 187-93. PMID 7796053 DOI: 10.1016/0968-0896(95)00013-7  0.394
1995 Groutas WC, Venkataraman R, Chong LS, Yoder JE, Epp JB, Stanga MA, Kim EH. Isoxazoline derivatives as potential inhibitors of the proteolytic enzymes human leukocyte elastase, cathepsin G and proteinase 3: a structure-activity relationship study. Bioorganic & Medicinal Chemistry. 3: 125-8. PMID 7796046 DOI: 10.1016/0968-0896(95)00006-3  0.354
1995 Groutas WC, Venkataraman R, Kuang R. Catalysis in Drug Design and Medicinal Chemistry Transactions of the Kansas Academy of Science (1903-). 98: 17. DOI: 10.2307/3628075  0.47
1994 Groutas WC, Kuang R, Venkataraman R. Substituted 3-oxo-1,2,5-thiadiazolidine 1,1-dioxides: A new class of potential mechanism-based inhibitors of human leukocyte elastase and cathepsin G Biochemical and Biophysical Research Communications. 198: 341-349. PMID 8292039 DOI: 10.1006/Bbrc.1994.1048  0.463
1994 Groutas WC, Huang H, Venkataraman R, Houser-Archield N, Epp JB. Dual-action inhibitors of proteolytic enzymes: potential therapeutic agents for cystic fibrosis and related ailments. Bioorganic & Medicinal Chemistry. 1: 273-7. PMID 8081858 DOI: 10.1016/S0968-0896(00)82132-X  0.306
1993 Groutas WC, Chong LS, Venkataraman R, Epp JB, Kuang RZ, Brubaker MJ, Houser-Archield N, Huang H, McClenahan JJ. Mechanism-based inhibitors of serine proteinases based on the Gabriel-Colman rearrangement. Biochemical and Biophysical Research Communications. 194: 1491-9. PMID 8352807 DOI: 10.1006/bbrc.1993.1993  0.397
1993 Groutas WC, Venkataraman R, Brubaker MJ, Epp JB, Chong LS, Stanga MA, McClenahan JJ, Tagusagawa F. 3-(Alkylthio)-N-hydroxysuccinimide derivatives: potent inhibitors of human leukocyte elastase. Biochimica Et Biophysica Acta. 1164: 283-8. PMID 8343527 DOI: 10.1016/0167-4838(93)90260-X  0.376
1993 Groutas WC, Chong LS, Venkataraman R. Novel potential mechanism-based inhibitors of human leukocyte elastase and cathepsin G: derivatives of isothiazolidin-3-one. Biochemical and Biophysical Research Communications. 197: 730-9. PMID 8267609 DOI: 10.1006/Bbrc.1993.2540  0.482
1993 Groutas WC, Houser-Archield N, Chong LS, Venkataraman R, Epp JB, Huang H, McClenahan JJ. Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives. Journal of Medicinal Chemistry. 36: 3178-81. PMID 8230105 DOI: 10.1021/JM00073A019  0.333
1993 Groutas WC, Chong LS, Venkataraman R, Huang H, Epp JB, Kuang R. A general approach toward the design of mechanism-based inactivators of serine proteinases: inactivation of human leukocyte elastase by a phthalimide derivative Bioorganic and Medicinal Chemistry Letters. 3: 2745-2750. DOI: 10.1016/S0960-894X(01)80756-3  0.388
1993 Groutas WC, Castrisos JC, Stanga MA, Kuang Rz, Venkataraman R, Epp JB, Brubaker MJ, Chong LS. Heterocyclic inhibitors of human leukocyte elastase: 3-Hydroxypyridazopyrimidine, 3-hydroxypyridopyrimidine and 3-hydroxyquinazoline-2,4-1H,3H0dione derivatives Bioorganic and Medicinal Chemistry Letters. 3: 1163-1168. DOI: 10.1016/S0960-894X(00)80307-8  0.372
1992 Groutas WC, Brubaker MJ, Venkataraman R, Epp JB, Stanga MA, McClenahan JJ. Inhibitors of human neutrophil cathepsin G: structural and biochemical studies. Archives of Biochemistry and Biophysics. 294: 144-6. PMID 1497704 DOI: 10.1016/0003-9861(92)90148-P  0.476
1992 Brubaker MJ, Groutas WC, Hoidal JR, Rao NV. Human neutrophil proteinase 3: Mapping of the substrate binding site using peptidyl thiobenzyl esters Biochemical and Biophysical Research Communications. 188: 1318-1324. PMID 1445363 DOI: 10.1016/0006-291X(92)91375-Z  0.321
1992 Groutas WC, Brubaker MJ, Venkataraman R, Epp JB, Houser-Archield N, Chong LS, McClenahan JJ. Potential mechanism-based inhibitors of proteolytic enzymes Bioorganic and Medicinal Chemistry Letters. 2: 175-180. DOI: 10.1016/S0960-894X(01)80445-5  0.529
1992 Groutas WC, Chong LS, Epp JB, Venkataraman R, Brubaker MJ, Stanga MA, Kim EH, Keller CE. Inhibition of human leukocyte elastase and cathepsin G by isoxazoline derivatives Bioorganic and Medicinal Chemistry Letters. 2: 1571-1574. DOI: 10.1016/S0960-894X(00)80432-1  0.367
1992 Groutas WC, Huang H, Epp JB, Brubaker MJ, Keller CE, McClenahan JJ. A general approach toward the design of inhibitors of serine proteinases: inhibition of human leukocyte elastase by substituted dihydrouracils Bioorganic and Medicinal Chemistry Letters. 2: 1565-1570. DOI: 10.1016/S0960-894X(00)80431-X  0.449
1991 Groutas WC, Venkataraman R, Brubaker MJ, Stanga MA. Inhibition of human leukocyte elastase by phosphate esters of N-hydroxysuccinimide and its derivatives: direct observation of a phosphorylated enzyme by 31P nuclear magnetic resonance spectroscopy. Biochemistry. 30: 4132-6. PMID 2021604 DOI: 10.1021/Bi00231A004  0.459
1990 Groutas WC, Hoidal JR, Brubaker MJ, Stanga MA, Venkataraman R, Gray BH, Rao NV. Inhibitors of human leukocyte proteinase-3. Journal of Medicinal Chemistry. 33: 1085-7. PMID 2319555 DOI: 10.1021/Jm00166A001  0.435
1990 Groutas WC, Stanga MA, Castrisos JC, Schatz EJ, Brubaker MJ. Ionic inhibitors of human leukocyte elastase: Pyridinium and phenyl carboxylate derivatives of 3-alkyl-N-hydroxysuccinimide Journal of Pharmaceutical Sciences. 79: 886-888. PMID 2280356 DOI: 10.1002/Jps.2600791008  0.444
1990 Groutas WC, Stanga MA, Castrisos JC, Schatz EJ. Hydantoin derivatives. A new class of inhibitors of human leukocyte elastase Journal of Enzyme Inhibition and Medicinal Chemistry. 3: 237-243. PMID 2079641 DOI: 10.3109/14756369009035842  0.43
1989 Groutas WC, Brubaker MJ, Stanga MA, Castrisos JC, Crowley JP, Schatz EJ. Inhibition of human leukocyte elastase by derivatives of N-hydroxysuccinimide. A structure-activity-relationship study Journal of Medicinal Chemistry. 32: 1607-1611. PMID 2738894 DOI: 10.1021/Jm00127A034  0.483
1987 Groutas WC, Brubaker MJ, Zandler ME, Mazo-Gray V, Rude SA, Crowley JP, Castrisos JC, Dunshee DA, Giri PK. Inactivation of leukocyte elastase by aryl azolides and sulfonate salts. Structure-activity relationship studies. Journal of Medicinal Chemistry. 29: 1302-5. PMID 3643283 DOI: 10.1021/Jm00157A034  0.441
1987 Groutas WC. Inhibitors of leukocyte elastase and leukocyte cathepsin G. Agents for the treatment of emphysema and related ailments. Medicinal Research Reviews. 7: 227-41. PMID 3553781 DOI: 10.1002/Med.2610070205  0.366
1986 Groutas WC, Giri PK, Crowley JP, Castrisos JC, Brubaker MJ. The lossen rearrangement in biological systems. inactivation of leukocyte elastase and alpha-chymotrypsin by (DL)-3-benzyl-N- (methanesulfonyloxy) succinimide Biochemical and Biophysical Research Communications. 141: 741-748. PMID 3643025 DOI: 10.1016/S0006-291X(86)80235-2  0.391
1985 Groutas WC, Brubaker MJ, Zandler ME, Stanga MA, Huang TL, Castrisos JC, Crowley JP. Sulfonate salts of amino acids: novel inhibitors of the serine proteinases. Biochemical and Biophysical Research Communications. 128: 90-3. PMID 3885950 DOI: 10.1016/0006-291X(85)91648-1  0.394
1985 Groutas WC, Stanga MA, Brubaker MJ, Huang TL, Moi MK, Carroll RT. Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases Journal of Medicinal Chemistry. 28: 1106-1109. PMID 3848491 DOI: 10.1021/JM00146A023  0.388
1985 Groutas WC, Abrams WR, Theodorakis MC, Kasper AM, Rude SA, Badger RC, Ocain TD, Miller KE, Moi MK, Brubaker MJ. Amino acid derived latent isocyanates: irreversible inactivation of porcine pancreatic elastase and human leukocyte elastase. Journal of Medicinal Chemistry. 28: 204-9. PMID 3844034 DOI: 10.1002/Chin.198524212  0.383
1985 Groutas WC, Huang TL, Stanga MA, Brubaker MJ, Moi MK. Substituted 2-Pyrones and 5,6-Dihydropyrones Journal of Heterocyclic Chemistry. 22: 433-435. DOI: 10.1002/Jhet.5570220243  0.39
1985 GROUTAS WC, HUANG TL, STANGA MA, BRUBAKER MJ, MOI MK. ChemInform Abstract: SUBSTITUTED 2-PYRONES AND 5,6-DIHYDROPYRONES AS INHIBITORS OF THE SERINE PROTEASES Chemischer Informationsdienst. 16. DOI: 10.1002/Chin.198546160  0.339
1984 Groutas WC, Abrams WR, Carroll RT, Moi MK, Miller KE, Margolis MT. Specific inhibition of human leukocyte elastase by substituted alpha-pyrones. Experientia. 40: 361-2. PMID 6562017 DOI: 10.1007/Bf01952552  0.426
1980 Groutas WC, Badger RC, Ocain TD, Felker D, Frankson J, Theodorakis M. Mechanism-based inhibitors of elastase. Biochemical and Biophysical Research Communications. 95: 1890-4. PMID 6903133 DOI: 10.1016/S0006-291X(80)80120-3  0.336
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