Darren W. Engers, Ph.D. - Publications

Affiliations: 
2006 University of Texas at Austin, Austin, Texas, U.S.A. 
Area:
Organic Chemistry

64 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
2021 Spock M, Carter TR, Bollinger KA, Han C, Baker LA, Rodriguez AL, Peng L, Dickerson JW, Qi A, Rook JM, O'Neill JC, Watson KJ, Chang S, Bridges TM, Engers JL, ... Engers DW, et al. Discovery of VU6028418: A Highly Selective and Orally Bioavailable M Muscarinic Acetylcholine Receptor Antagonist. Acs Medicinal Chemistry Letters. 12: 1342-1349. PMID 34413964 DOI: 10.1021/acsmedchemlett.1c00363  1
2021 Spearing PK, Cho HP, Luscombe VB, Blobaum AL, Boutaud O, Engers DW, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Bender AM. Discovery of a Novel Class of Heteroaryl-Pyrrolidinones as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M. Bioorganic & Medicinal Chemistry Letters. 128193. PMID 34118412 DOI: 10.1016/j.bmcl.2021.128193  1
2020 Engers DW, Bollinger SR, Felts AS, Vadukoot AK, Williams CH, Blobaum AL, Lindsley CW, Hong CC, Hopkins CR. Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors. Bioorganic & Medicinal Chemistry Letters. 30: 127418. PMID 32750526 DOI: 10.1016/J.Bmcl.2020.127418  1
2019 Temple KJ, Long MF, Engers JL, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Jeffrey Conn P, Engers DW, Lindsley CW. Discovery of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypes. Bioorganic & Medicinal Chemistry Letters. 126811. PMID 31787491 DOI: 10.1016/J.Bmcl.2019.126811  1
2019 Temple KJ, Engers JL, Long MF, Watson KJ, Chang S, Luscombe VB, Jenkins MT, Rodriguez AL, Niswender CM, Bridges TM, Jeffrey Conn P, Engers DW, Lindsley CW. Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M positive allosteric modulator (PAM) chemotype. Bioorganic & Medicinal Chemistry Letters. 126812. PMID 31784320 DOI: 10.1016/J.Bmcl.2019.126812  1
2019 Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Discovery of a novel 3,4-dimethylcinnoline carboxamide M positive allosteric modulator (PAM) chemotype via scaffold hopping. Bioorganic & Medicinal Chemistry Letters. 126678. PMID 31537424 DOI: 10.1016/j.bmcl.2019.126678  1
2019 Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, et al. SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M PAMs. Bioorganic & Medicinal Chemistry Letters. PMID 31248774 DOI: 10.1016/J.Bmcl.2019.06.032  1
2019 Kharade SV, Sanchez-Andres JV, Fulton MG, Shelton EJ, Blobaum AL, Engers DW, Hofmann CS, Dadi PK, Lantier L, Jacobson DA, Lindsley CW, Denton JS. Structure-activity relationships, pharmacokinetics, and pharmacodynamics of the Kir6.2/SUR1-specific channel opener, VU0071063. The Journal of Pharmacology and Experimental Therapeutics. PMID 31201216 DOI: 10.1124/Jpet.119.257204  1
2019 Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, et al. VU6005806/AZN-00016130, an advanced M positive allosteric modulator (PAM) profiled as a potential preclinical development candidate. Bioorganic & Medicinal Chemistry Letters. PMID 31113706 DOI: 10.1016/J.Bmcl.2019.05.026  1
2019 Iwaki Y, Yashiro K, Kokubo M, Mori T, Wieting JM, McGowan KM, Bridges TM, Engers DW, Denton JS, Kurata H, Lindsley CW. Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249. Bioorganic & Medicinal Chemistry Letters. PMID 31072652 DOI: 10.1016/J.Bmcl.2019.04.048  1
2019 Maksymetz J, Joffe ME, Moran SP, Stansley BJ, Li B, Temple K, Engers DW, Lawrence JJ, Lindsley CW, Conn PJ. M Muscarinic Receptors Modulate Fear-Related Inputs to the Prefrontal Cortex: Implications for Novel Treatments of Posttraumatic Stress Disorder. Biological Psychiatry. PMID 31003787 DOI: 10.1016/J.Biopsych.2019.02.020  1
2019 Reed CW, Washecheck JP, Quitlag MC, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Jeffrey Conn P, Niswender CM, Lindsley CW. Surveying heterocycles as amide bioisosteres within a series of mGlu NAMs: Discovery of VU6019278. Bioorganic & Medicinal Chemistry Letters. PMID 30910459 DOI: 10.1016/J.Bmcl.2019.03.016  1
2019 Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, et al. Discovery of VU2957 (Valiglurax): An mGlu Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease. Acs Medicinal Chemistry Letters. 10: 255-260. PMID 30891122 DOI: 10.1021/Acsmedchemlett.8B00426  1
2019 Reed CW, Yohn S, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Discovery of an orally bioavailable and Central Nervous System (CNS) penetrant mGlu7 Negative Allosteric Modulator (NAM) in vivo tool compound: N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962). Journal of Medicinal Chemistry. PMID 30608678 DOI: 10.1021/Acs.Jmedchem.8B01810  1
2018 Poslusney MS, Salovich JM, Wood MR, Melancon BJ, Bollinger KA, Luscombe VB, Rodriguez AL, Engers DW, Bridges TM, Niswender CM, Jeffrey Conn P, Lindsley CW. Novel M positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands. Bioorganic & Medicinal Chemistry Letters. PMID 30580918 DOI: 10.1016/J.Bmcl.2018.12.039  1
2018 Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, et al. The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu PAM development candidate. Bioorganic & Medicinal Chemistry Letters. PMID 30503632 DOI: 10.1016/J.Bmcl.2018.10.050  1
2018 Engers JL, Childress ES, Long MF, Capstick RA, Luscombe VB, Cho HP, Dickerson JW, Rook JM, Blobaum AL, Niswender CM, Engers DW, Conn PJ, Lindsley CW. VU6007477, a Novel M PAM Based on a Pyrrolo[2,3-]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events. Acs Medicinal Chemistry Letters. 9: 917-922. PMID 30258541 DOI: 10.1021/Acsmedchemlett.8B00261  1
2018 Bollinger S, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. The discovery, SAR and biological characterization of a novel series of 6-((1H-pyrazolo[4,3-b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Journal of Medicinal Chemistry. PMID 30247901 DOI: 10.1021/Acs.Jmedchem.8B00994  1
2018 Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, et al. Corrigendum to "Challenges in the development of an M PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]. Bioorganic & Medicinal Chemistry Letters. PMID 30076050 DOI: 10.1016/J.Bmcl.2018.07.022  1
2018 Engers DW, Bollinger SR, Engers JL, Panarese JD, Breiner MM, Gregro A, Blobaum AL, Bronson JJ, Wu YJ, Macor JE, Rodriguez AL, Zamorano R, Conn PJ, Lindsley CW, Niswender CM, et al. Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu positive allosteric modulators that mitigate CYP1A2 induction liability. Bioorganic & Medicinal Chemistry Letters. PMID 29958762 DOI: 10.1016/J.Bmcl.2018.06.034  1
2018 Bertron JL, Cho HP, Garcia-Barrantes PM, Panarese JD, Salovich JM, Nance KD, Engers DW, Rook JM, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. The discovery of VU0486846: steep SAR from a series of M PAMs based on a novel benzomorpholine core. Bioorganic & Medicinal Chemistry Letters. PMID 29754948 DOI: 10.1016/J.Bmcl.2018.05.009  1
2018 Moran SP, Dickerson JW, Cho HP, Xiang Z, Maksymetz J, Remke DH, Lv X, Doyle CA, Rajan DH, Niswender CM, Engers DW, Lindsley CW, Rook JM, Conn PJ. M-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 29581537 DOI: 10.1038/S41386-018-0033-9  1
2017 Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, et al. Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides. Bioorganic & Medicinal Chemistry Letters. PMID 29089231 DOI: 10.1016/J.Bmcl.2017.10.053  1
2017 Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, et al. Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. Acs Medicinal Chemistry Letters. 8: 1110-1115. PMID 29057060 DOI: 10.1021/Acsmedchemlett.7B00317  1
2017 Long MF, Engers JL, Chang S, Zhan X, Weiner RL, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW. Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping. Bioorganic & Medicinal Chemistry Letters. PMID 29037946 DOI: 10.1016/J.Bmcl.2017.10.016  1
2017 Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW. Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core. Bioorganic & Medicinal Chemistry Letters. PMID 28866269 DOI: 10.1016/J.Bmcl.2017.08.043  1
2017 Gogliotti RG, Senter RK, Fisher NM, Adams J, Zamorano R, Walker AG, Blobaum AL, Engers DW, Hopkin CR, Daniels JS, Jones CK, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome. Science Translational Medicine. 9. PMID 28814546 DOI: 10.1126/Scitranslmed.Aai7459  1
2017 Bender AM, Weiner RL, Luscombe VB, Ajmera S, Cho HP, Chang S, Zhan X, Rodriguez AL, Niswender CM, Engers DW, Bridges TM, Conn PJ, Lindsley CW. Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. Bioorganic & Medicinal Chemistry Letters. PMID 28633897 DOI: 10.1016/J.Bmcl.2017.05.042  1
2017 Melancon BJ, Wood MR, Noetzel MJ, Nance KD, Engelberg EM, Han C, Lamsal A, Chang S, Cho HP, Byers FW, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, et al. Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology. Bioorganic & Medicinal Chemistry Letters. PMID 28442253 DOI: 10.1016/J.Bmcl.2017.04.043  1
2017 Bender AM, Weiner RL, Luscombe VB, Cho HP, Niswender CM, Engers DW, Bridges TM, Jeffrey Conn P, Lindsley CW. Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype. Bioorganic & Medicinal Chemistry Letters. PMID 28427812 DOI: 10.1016/J.Bmcl.2017.04.009  1
2017 Wood MR, Noetzel MJ, Melancon BJ, Poslusney MS, Nance KD, Hurtado MA, Luscombe VB, Weiner RL, Rodriguez AL, Lamsal A, Chang S, Bubser M, Blobaum AL, Engers DW, Niswender CM, et al. Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. Acs Medicinal Chemistry Letters. 8: 233-238. PMID 28197318 DOI: 10.1021/Acsmedchemlett.6B00461  1
2016 Rook JM, Abe M, Cho HP, Nance KD, Luscombe VB, Adams JJ, Dickerson JW, Remke DH, Garcia-Barrantes PM, Engers DW, Engers JL, Chang S, Foster JJ, Blobaum AL, Niswender CM, et al. Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs. Acs Chemical Neuroscience. PMID 28001356 DOI: 10.1021/Acschemneuro.6B00429  1
2016 Wood MR, Noetzel MJ, Poslusney MS, Melancon BJ, Tarr JC, Lamsal A, Chang S, Luscombe VB, Weiner RL, Cho HP, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, et al. Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs. Bioorganic & Medicinal Chemistry Letters. PMID 27939174 DOI: 10.1016/J.Bmcl.2016.11.086  1
2016 Swale DR, Engers DW, Bollinger SR, Gross A, Inocente EA, Days E, Kanga F, Johnson RM, Yang L, Bloomquist JR, Hopkins CR, Piermarini PM, Denton JS. An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria. Scientific Reports. 6: 36954. PMID 27849039 DOI: 10.1038/Srep36954  1
2016 Wood MR, Noetzel MJ, Tarr JC, Rodriguez AL, Lamsal A, Chang S, Foster JJ, Smith E, Chase P, Hodder PS, Engers DW, Niswender CM, Brandon NJ, Wood MW, Duggan ME, et al. Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition. Bioorganic & Medicinal Chemistry Letters. PMID 27476142 DOI: 10.1016/J.Bmcl.2016.07.042  1
2016 Niswender CM, Jones CK, Lin X, Bubser M, Thompson Gray A, Blobaum AL, Engers DW, Rodriguez AL, Loch MT, Daniels JS, Lindsley CW, Hopkins CR, Javitch JA, Conn PJ. Development and antiparkinsonian activity of VU0418506, a selective positive allosteric modulator of metabotropic glutamate receptor 4 homomers without activity at mGlu2/4 heteromers. Acs Chemical Neuroscience. PMID 27441572 DOI: 10.1021/Acschemneuro.6B00036  1
2016 Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy. Bioorganic & Medicinal Chemistry Letters. PMID 27131990 DOI: 10.1016/J.Bmcl.2016.04.041  1
2016 Engers DW, Blobaum AL, Gogliotti RD, Cheung YY, Salovich JM, Garcia-Barrantes PM, Daniels JS, Morrison R, Jones CK, Soars MG, Zhuo X, Hurley J, Macor JE, Bronson JJ, Conn PJ, et al. Discovery, Synthesis and Pre-Clinical Characterization of N-(3-chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4). Acs Chemical Neuroscience. PMID 27075300 DOI: 10.1021/Acschemneuro.6B00035  1
2015 Klar R, Walker AG, Ghose D, Grueter BA, Engers DW, Hopkins CR, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 35: 7600-15. PMID 25972184 DOI: 10.1523/Jneurosci.4543-14.2015  1
2015 Bollinger SR, Engers DW, Ennis EA, Wright J, Locuson CW, Lindsley CW, Blakely RD, Hopkins CR. Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. Bioorganic & Medicinal Chemistry Letters. 25: 1757-60. PMID 25801932 DOI: 10.1016/J.Bmcl.2015.02.058  1
2014 Hempel JE, Engers DW, Sulikowski GA. Synthetic studies directed toward the AB decalin common to HMP-Y1 and hibarimicinone. Tetrahedron Letters. 55: 2157-2159. PMID 32855575 DOI: 10.1016/J.Tetlet.2014.02.069  1
2014 Raphemot R, Rouhier MF, Swale DR, Days E, Weaver CD, Lovell KM, Konkel LC, Engers DW, Bollinger SR, Bollinger SF, Hopkins C, Piermarini PM, Denton JS. Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels. Plos One. 9: e110772. PMID 25375326 DOI: 10.1371/Journal.Pone.0110772  1
2014 Tsugawa D, Oya Y, Masuzaki R, Ray K, Engers DW, Dib M, Do N, Kuramitsu K, Ho K, Frist A, Yu PB, Bloch KD, Lindsley CW, Hopkins CR, Hong CC, et al. Specific activin receptor-like kinase 3 inhibitors enhance liver regeneration. The Journal of Pharmacology and Experimental Therapeutics. 351: 549-58. PMID 25271257 DOI: 10.1124/Jpet.114.216903  1
2014 Jalan-Sakrikar N, Field JR, Klar R, Mattmann ME, Gregory KJ, Zamorano R, Engers DW, Bollinger SR, Weaver CD, Days EL, Lewis LM, Utley TJ, Hurtado M, Rigault D, Acher F, et al. Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7. Acs Chemical Neuroscience. 5: 1221-37. PMID 25225882 DOI: 10.1021/Cn500153Z  1
2014 Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL. A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors. Acs Chemical Neuroscience. 5: 597-610. PMID 24798819 DOI: 10.1021/Cn5000343  1
2014 Hempel JE, Engers DW, Sulikowski GA. Synthetic studies directed toward the AB decalin common to HMP-Y1 and hibarimicinone Tetrahedron Letters. 55: 2157-2159. DOI: 10.1016/j.tetlet.2014.02.069  1
2013 Engers DW, Lindsley CW. Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders. Drug Discovery Today. Technologies. 10: e269-76. PMID 24050278 DOI: 10.1016/J.Ddtec.2012.10.007  1
2013 Ramos-Hunter SJ, Engers DW, Kaufmann K, Du Y, Lindsley CW, Weaver CD, Sulikowski GA. Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators. Bioorganic & Medicinal Chemistry Letters. 23: 5195-8. PMID 23916258 DOI: 10.1016/J.Bmcl.2013.07.002  1
2013 Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR. Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorganic & Medicinal Chemistry Letters. 23: 3248-52. PMID 23639540 DOI: 10.1016/J.Bmcl.2013.03.113  1
2012 Potet F, Lorinc AN, Chaigne S, Hopkins CR, Venkataraman R, Stepanovic SZ, Lewis LM, Days E, Sidorov VY, Engers DW, Zou B, Afshartous D, George AL, Campbell CM, Balser JR, et al. Identification and characterization of a compound that protects cardiac tissue from human Ether-à-go-go-related gene (hERG)-related drug-induced arrhythmias. The Journal of Biological Chemistry. 287: 39613-25. PMID 23033485 DOI: 10.1074/Jbc.M112.380162  1
2012 Mattmann ME, Yu H, Lin Z, Xu K, Huang X, Long S, Wu M, McManus OB, Engers DW, Le UM, Li M, Lindsley CW, Hopkins CR. Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator. Bioorganic & Medicinal Chemistry Letters. 22: 5936-41. PMID 22910039 DOI: 10.1016/J.Bmcl.2012.07.060  1
2012 Jones CK, Bubser M, Thompson AD, Dickerson JW, Turle-Lorenzo N, Amalric M, Blobaum AL, Bridges TM, Morrison RD, Jadhav S, Engers DW, Italiano K, Bode J, Daniels JS, Lindsley CW, et al. The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease. The Journal of Pharmacology and Experimental Therapeutics. 340: 404-21. PMID 22088953 DOI: 10.1124/Jpet.111.187443  1
2011 Robichaud AJ, Engers DW, Lindsley CW, Hopkins CR. Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics. Acs Chemical Neuroscience. 2: 433-49. PMID 22860170 DOI: 10.1021/Cn200043E  1
2011 Jones CK, Engers DW, Thompson AD, Field JR, Blobaum AL, Lindsley SR, Zhou Y, Gogliotti RD, Jadhav S, Zamorano R, Bogenpohl J, Smith Y, Morrison R, Daniels JS, Weaver CD, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model. Journal of Medicinal Chemistry. 54: 7639-47. PMID 21966889 DOI: 10.1021/Jm200956Q  1
2011 Wang HR, Wu M, Yu H, Long S, Stevens A, Engers DW, Sackin H, Daniels JS, Dawson ES, Hopkins CR, Lindsley CW, Li M, McManus OB. Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133. Acs Chemical Biology. 6: 845-56. PMID 21615117 DOI: 10.1021/Cb200146A  1
2011 Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. Journal of Medicinal Chemistry. 54: 1106-10. PMID 21247167 DOI: 10.1021/Jm101271S  1
2011 Lamb JP, Engers DW, Niswender CM, Rodriguez AL, Venable DF, Conn PJ, Lindsley CW. Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists. Bioorganic & Medicinal Chemistry Letters. 21: 2711-4. PMID 21183344 DOI: 10.1016/J.Bmcl.2010.11.119  1
2010 Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chemistry Letters. 20: 5175-8. PMID 20667732 DOI: 10.1016/J.Bmcl.2010.07.007  1
2009 Lindsley CW, Niswender CM, Engers DW, Hopkins CR. Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease. Current Topics in Medicinal Chemistry. 9: 949-63. PMID 19754407 DOI: 10.2174/156802609789378272  1
2009 Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). Journal of Medicinal Chemistry. 52: 4115-8. PMID 19469556 DOI: 10.1021/Jm9005065  1
2009 Engers DW, Rodriguez AL, Williams R, Hammond AS, Venable D, Oluwatola O, Sulikowski GA, Conn PJ, Lindsley CW. Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273. Chemmedchem. 4: 505-11. PMID 19197923 DOI: 10.1002/Cmdc.200800357  1
2007 Zhao H, Engers DW, Morales CL, Pagenkopf BL. Reactions of alanes and aluminates with tri-substituted epoxides. Development of a stereospecific alkynylation at the more hindered carbon Tetrahedron. 63: 8774-8780. DOI: 10.1016/J.Tet.2007.06.036  1
2005 Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, ... ... Engers D, et al. Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase. Bioorganic & Medicinal Chemistry. 13: 2859-72. PMID 15781396 DOI: 10.1016/j.bmc.2005.02.014  0.01
2004 Engers DW, Bassindale MJ, Pagenkopf BL. Synthesis of the C(1)-C(12) segment of peloruside A by an alpha-benzyloxymethyl ketone aldol strategy. Organic Letters. 6: 663-6. PMID 14986944 DOI: 10.1021/Ol036393Z  1
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