Year |
Citation |
Score |
2019 |
Schnute ME, Benoit SE, Buchler IP, Caspers N, Grapperhaus ML, Han S, Hotchandani R, Huang N, Hughes RO, Juba BM, Kim KH, Liu E, McCarthy E, Messing D, Miyashiro JS, ... ... Walker DP, et al. Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. Acs Medicinal Chemistry Letters. 10: 80-85. PMID 30655951 DOI: 10.1021/Acsmedchemlett.8B00461 |
0.332 |
|
2019 |
Walker DP, Harris GD, Carroll JN, Boehm TL, McReynolds MD, Struble JR, van Herpt J, van Zwieten D, Koeller KJ, Bore M. A new process to prepare 3,6-dichloro-2-hydroxybenzoic acid, the penultimate intermediate in the synthesis of herbicide dicamba Tetrahedron Letters. 60: 1032-1036. DOI: 10.1016/J.Tetlet.2019.03.024 |
0.301 |
|
2017 |
Stepan AF, Claffey MM, Reese MR, Balan G, Barreiro G, Barricklow J, Bohanon MJ, Boscoe BP, Cappon GD, Chenard LK, Cianfrogna J, Chen L, Coffman KJ, Drozda SE, Dunetz JR, ... ... Walker DP, et al. Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Non-human Primates. Journal of Medicinal Chemistry. PMID 28817277 DOI: 10.1021/Acs.Jmedchem.7B00604 |
0.325 |
|
2015 |
Blount KF, Megyola C, Plummer M, Osterman D, O'Connell T, Aristoff P, Quinn C, Chrusciel RA, Poel TJ, Schostarez HJ, Stewart CA, Walker DP, Wuts PG, Breaker RR. Novel Riboswitch-Binding Flavin Analog That Protects Mice against Clostridium difficile Infection without Inhibiting Cecal Flora. Antimicrobial Agents and Chemotherapy. 59: 5736-46. PMID 26169403 DOI: 10.1128/Aac.01282-15 |
0.314 |
|
2014 |
Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, ... ... Walker DP, et al. Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator. Journal of Medicinal Chemistry. 57: 861-77. PMID 24392688 DOI: 10.1021/Jm401622K |
0.351 |
|
2013 |
Daniels JS, Lai Y, South S, Chiang PC, Walker D, Feng B, Mireles R, Whiteley LO, McKenzie JW, Stevens J, Mourey R, Anderson D, Davis Ii JW. Inhibition of hepatobiliary transporters by a novel kinase inhibitor contributes to hepatotoxicity in beagle dogs. Drug Metabolism Letters. 7: 15-22. PMID 24138031 DOI: 10.2174/18723128112066660018 |
0.317 |
|
2013 |
Walker DP, Arhancet GB, Lu HF, Heasley SE, Metz S, Kablaoui NM, Franco FM, Hanau CE, Scholten JA, Springer JR, Fobian YM, Carter JS, Xing L, Yang S, Shaffer AF, et al. Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design. Bioorganic & Medicinal Chemistry Letters. 23: 1120-6. PMID 23298810 DOI: 10.1016/J.Bmcl.2012.11.107 |
0.393 |
|
2013 |
Arhancet GB, Walker DP, Metz S, Fobian YM, Heasley SE, Carter JS, Springer JR, Jones DE, Hayes MJ, Shaffer AF, Jerome GM, Baratta MT, Zweifel B, Moore WM, Masferrer JL, et al. Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation. Bioorganic & Medicinal Chemistry Letters. 23: 1114-9. PMID 23260349 DOI: 10.1016/J.Bmcl.2012.11.109 |
0.407 |
|
2013 |
Walker DP, Rogier DJ. Preparation of Novel Bridged Bicyclic Thiomorpholines as Potentially Useful Building Blocks in Medicinal Chemistry Synthesis. 45: 2966-2970. DOI: 10.1055/S-0033-1338528 |
0.35 |
|
2012 |
Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS, Griffith DA, Griffor MC, Guimarães CR, Guzman-Perez A, Han S, ... ... Walker DP, et al. Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors. Bioorganic & Medicinal Chemistry Letters. 22: 7523-9. PMID 23153798 DOI: 10.1016/J.Bmcl.2012.10.039 |
0.343 |
|
2012 |
Walker DP, Eklov BM, Bedore MW. Practical synthesis of 3-oxa-6-azabicyclo[31.1]heptane hydrotosylate; A novel morpholine-based building block Synthesis (Germany). 44: 2859-2862. DOI: 10.1055/S-0032-1316748 |
0.353 |
|
2012 |
Walker DP, Bedore MW. Concise synthesis of N 3- and N 6-monoprotected 3,6-diazabicyclo[3.1.1]heptanes; Useful intermediates for the preparation of novel bridged bicyclic piperazines Tetrahedron Letters. 53: 6332-6334. DOI: 10.1016/J.Tetlet.2012.08.156 |
0.332 |
|
2011 |
Walker DP, Heasley SE, MacInnes A, Anjeh T, Lu HF, Fobian YM, Collins JT, Vazquez ML, Mao MK. A practical synthesis of [(1 S,3 S)-3-aminocyclohexyl]methanol and 2-[(1 S,3 S)-3-aminocyclohexyl]propan-2-ol, useful intermediates for the preparation of novel m PGES-1 inhibitors Synlett. 2959-2962. DOI: 10.1055/S-0031-1289884 |
0.313 |
|
2011 |
Wishka DG, Beagley P, Lyon J, Farley KA, Walker DP. A concise synthesis of 6-oxa-3-azabicyclo[31.1]heptane hydrotosylate Synthesis. 2619-2624. DOI: 10.1055/S-0030-1260116 |
0.352 |
|
2011 |
Wishka DG, Walker DP. Synthesis of (±)-6-oxa-3-azabicyclo[3.1.1]heptan-2-thione: A potential synthon for the preparation of novel heteroaryl-annulated bicyclic morpholines Tetrahedron Letters. 52: 4713-4715. DOI: 10.1016/J.Tetlet.2011.07.017 |
0.322 |
|
2010 |
Kalgutkar AS, Griffith DA, Ryder T, Sun H, Miao Z, Bauman JN, Didiuk MT, Frederick KS, Zhao SX, Prakash C, Soglia JR, Bagley SW, Bechle BM, Kelley RM, Dirico K, ... ... Walker DP, et al. Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis. Chemical Research in Toxicology. 23: 1115-26. PMID 20507089 DOI: 10.1021/Tx100137N |
0.352 |
|
2010 |
Walker DP, Strohbach JW, McGlynn MA, Lu HF. A practical and stereoselective synthesis of (+/-)-trans-4- benzyloctahydropyrrolo[3,4-b][1,4]oxazine Journal of Heterocyclic Chemistry. 47: 1095-1103. DOI: 10.1002/Jhet.476 |
0.349 |
|
2009 |
Didiuk MT, Griffith DA, Benbow JW, Liu KK, Walker DP, Bi FC, Morris J, Guzman-Perez A, Gao H, Bechle BM, Kelley RM, Yang X, Dirico K, Ahmed S, Hungerford W, et al. Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 19: 4555-9. PMID 19625189 DOI: 10.1016/J.Bmcl.2009.07.004 |
0.34 |
|
2009 |
Walker DP, Zawistoski MP, McGlynn MA, Li JC, Kung DW, Bonnette PC, Baumann A, Buckbinder L, Houser JA, Boer J, Mistry A, Han S, Xing L, Guzman-Perez A. Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity. Bioorganic & Medicinal Chemistry Letters. 19: 3253-8. PMID 19428251 DOI: 10.1016/J.Bmcl.2009.04.093 |
0.403 |
|
2009 |
Boyer D, Bauman JN, Walker DP, Kapinos B, Karki K, Kalgutkar AS. Utility of metaSite in improving metabolic stability of the neutral indomethacin amide derivative and selective cyclooxygenase-2 inhibitor 2-(1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-A/-phenethyl-acetamide Drug Metabolism and Disposition. 37: 999-1008. PMID 19196840 DOI: 10.1124/Dmd.108.026112 |
0.355 |
|
2008 |
Walker DP, Bi FC, Kalgutkar AS, Bauman JN, Zhao SX, Soglia JR, Aspnes GE, Kung DW, Klug-McLeod J, Zawistoski MP, McGlynn MA, Oliver R, Dunn M, Li JC, Richter DT, et al. Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation. Bioorganic & Medicinal Chemistry Letters. 18: 6071-7. PMID 18951788 DOI: 10.1016/J.Bmcl.2008.10.030 |
0.407 |
|
2008 |
Acker BA, Jacobsen EJ, Rogers BN, Wishka DG, Reitz SC, Piotrowski DW, Myers JK, Wolfe ML, Groppi VE, Thornburgh BA, Tinholt PM, Walters RR, Olson BA, Fitzgerald L, Staton BA, ... ... Walker DP, et al. Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity. Bioorganic & Medicinal Chemistry Letters. 18: 3611-5. PMID 18490160 DOI: 10.1016/J.Bmcl.2008.04.070 |
0.349 |
|
2008 |
Walker DP, Acker BA, Jon Jacobsen E, Wishka DG. Preparation of novel azabicyclic amines and α7 nicotinic acetylcholine receptor activity of derived aryl amides Journal of Heterocyclic Chemistry. 45: 247-257. DOI: 10.1002/Jhet.5570450131 |
0.313 |
|
2006 |
Walker DP, Wishka DG, Piotrowski DW, Jia S, Reitz SC, Yates KM, Myers JK, Vetman TN, Margolis BJ, Jacobsen EJ, Acker BA, Groppi VE, Wolfe ML, Thornburgh BA, Tinholt PM, et al. Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as alpha7 nicotinic acetylcholine receptor agonists. Bioorganic & Medicinal Chemistry. 14: 8219-48. PMID 17011782 DOI: 10.1016/J.Bmc.2006.09.019 |
0.375 |
|
2006 |
Wishka DG, Walker DP, Yates KM, Reitz SC, Jia S, Myers JK, Olson KL, Jacobsen EJ, Wolfe ML, Groppi VE, Hanchar AJ, Thornburgh BA, Cortes-Burgos LA, Wong EH, Staton BA, et al. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. Journal of Medicinal Chemistry. 49: 4425-36. PMID 16821801 DOI: 10.1021/Jm0602413 |
0.331 |
|
1999 |
Walker DP, Grieco PA. Total synthesis of 5(R)- and 5(S)-polyandrane [11] Journal of the American Chemical Society. 121: 9891-9892. DOI: 10.1021/Ja992791E |
0.476 |
|
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