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Page 1
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
Cook J, Zusi FC, McDonald IM, King D, Hill MD, Iwuagwu C, Mate RA, Fang H, Zhao R, Wang B, Cutrone J, Ma B, Gao Q, Knox RJ, Matchett M, Gallagher L, Ferrante M, Post-Munson D, Molski T, Easton A, Miller R, Jones K, Digavalli S, Healy F, Lentz K, Benitex Y, Clarke W, Natale J, Siuciak JA, Lodge N, Zaczek R, Denton R, Morgan D, Bristow LJ, Macor JE, Olson RE. Cook J, et al. Among authors: zaczek r. J Med Chem. 2016 Dec 22;59(24):11171-11181. doi: 10.1021/acs.jmedchem.6b01506. Epub 2016 Dec 13. J Med Chem. 2016. PMID: 27958732
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE. Hartz RA, et al. Among authors: zaczek r. J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y. J Med Chem. 2009. PMID: 19552437
The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia.
Bristow LJ, Easton AE, Li YW, Sivarao DV, Lidge R, Jones KM, Post-Munson D, Daly C, Lodge NJ, Gallagher L, Molski T, Pieschl R, Chen P, Hendricson A, Westphal R, Cook J, Iwuagwu C, Morgan D, Benitex Y, King D, Macor JE, Zaczek R, Olson R. Bristow LJ, et al. Among authors: zaczek r. PLoS One. 2016 Jul 28;11(7):e0159996. doi: 10.1371/journal.pone.0159996. eCollection 2016. PLoS One. 2016. PMID: 27467081 Free PMC article.
Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] as α7 Nicotinic Receptor Agonists.
Hill MD, Fang H, King HD, Iwuagwu CI, McDonald IM, Cook J, Zusi FC, Mate RA, Knox RJ, Post-Munson D, Easton A, Miller R, Lentz K, Clarke W, Benitex Y, Lodge N, Zaczek R, Denton R, Morgan D, Bristow L, Macor JE, Olson R. Hill MD, et al. Among authors: zaczek r. ACS Med Chem Lett. 2016 Dec 1;8(1):133-137. doi: 10.1021/acsmedchemlett.6b00471. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105289 Free PMC article.
Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.
Iwuagwu C, King D, McDonald IM, Cook J, Zusi FC, Hill MD, Mate RA, Fang H, Knox R, Gallagher L, Post-Munson Amy Easton D, Miller R, Benitex Y, Siuciak J, Lodge N, Zaczek R, Morgan D, Bristow L, Macor JE, Olson RE. Iwuagwu C, et al. Among authors: zaczek r. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1261-1266. doi: 10.1016/j.bmcl.2017.01.058. Epub 2017 Jan 20. Bioorg Med Chem Lett. 2017. PMID: 28169167
BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
King D, Iwuagwu C, Cook J, McDonald IM, Mate R, Zusi FC, Hill MD, Fang H, Zhao R, Wang B, Easton AE, Miller R, Post-Munson D, Knox RJ, Gallagher L, Westphal R, Molski T, Fan J, Clarke W, Benitex Y, Lentz KA, Denton R, Morgan D, Zaczek R, Lodge NJ, Bristow LJ, Macor JE, Olson RE. King D, et al. Among authors: zaczek r. ACS Med Chem Lett. 2017 Feb 8;8(3):366-371. doi: 10.1021/acsmedchemlett.7b00032. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337332 Free PMC article.
Effects of BMS-902483, an α7 nicotinic acetylcholine receptor partial agonist, on cognition and sensory gating in relation to receptor occupancy in rodents.
Pieschl RL, Miller R, Jones KM, Post-Munson DJ, Chen P, Newberry K, Benitex Y, Molski T, Morgan D, McDonald IM, Macor JE, Olson RE, Asaka Y, Digavalli S, Easton A, Herrington J, Westphal RS, Lodge NJ, Zaczek R, Bristow LJ, Li YW. Pieschl RL, et al. Among authors: zaczek r. Eur J Pharmacol. 2017 Jul 15;807:1-11. doi: 10.1016/j.ejphar.2017.04.024. Epub 2017 Apr 22. Eur J Pharmacol. 2017. PMID: 28438647
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Dzierba CD, Sielecki TM, Arvanitis AG, Galka A, Johnson TL, Takvorian AG, Rafalski M, Kasireddy-Polam P, Vig S, Dasgupta B, Zhang G, Molski TF, Wong H, Zaczek RC, Lodge NJ, Combs AP, Gilligan PJ, Trainor GL, Bronson JJ, Macor JE. Dzierba CD, et al. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4986-9. doi: 10.1016/j.bmcl.2012.06.034. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22749422
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.
Hartz RA, Nanda KK, Ingalls CL, Ahuja VT, Molski TF, Zhang G, Wong H, Peng Y, Kelley M, Lodge NJ, Zaczek R, Gilligan PJ, Trainor GL. Hartz RA, et al. Among authors: zaczek r. J Med Chem. 2004 Sep 9;47(19):4741-54. doi: 10.1021/jm049787k. J Med Chem. 2004. PMID: 15341489
112 results