Darren W. Engers, Ph.D. - Publications

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

28 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
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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  0.88
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