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Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Chen CA, Jiang Y, Lu K, Daniewska I, Mazza CG, Negron L, Forray C, Parola T, Li B, Hegde LG, Wolinsky TD, Craig DA, Kong R, Wetzel JM, Andersen K, Marzabadi MR. Chen CA, et al. Among authors: wolinsky td. J Med Chem. 2007 Aug 9;50(16):3883-90. doi: 10.1021/jm060383x. J Med Chem. 2007. PMID: 17668922
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Jiang Y, Chen CA, Lu K, Daniewska I, De Leon J, Kong R, Forray C, Li B, Hegde LG, Wolinsky TD, Craig DA, Wetzel JM, Andersen K, Marzabadi MR. Jiang Y, et al. Among authors: wolinsky td. J Med Chem. 2007 Aug 9;50(16):3870-82. doi: 10.1021/jm060381c. J Med Chem. 2007. PMID: 17668921
Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder.
Packiarajan M, Marzabadi MR, Desai M, Lu Y, Noble SA, Wong WC, Jubian V, Chandrasena G, Wolinsky TD, Zhong H, Walker MW, Wiborg O, Andersen K. Packiarajan M, et al. Among authors: wolinsky td. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5436-41. doi: 10.1016/j.bmcl.2011.06.124. Epub 2011 Jul 2. Bioorg Med Chem Lett. 2011. PMID: 21782428
The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity.
Walker MW, Wolinsky TD, Jubian V, Chandrasena G, Zhong H, Huang X, Miller S, Hegde LG, Marsteller DA, Marzabadi MR, Papp M, Overstreet DH, Gerald CP, Craig DA. Walker MW, et al. Among authors: wolinsky td. J Pharmacol Exp Ther. 2009 Mar;328(3):900-11. doi: 10.1124/jpet.108.144634. Epub 2008 Dec 19. J Pharmacol Exp Ther. 2009. PMID: 19098165
Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299.
Swanson CJ, Blackburn TP, Zhang X, Zheng K, Xu ZQ, Hökfelt T, Wolinsky TD, Konkel MJ, Chen H, Zhong H, Walker MW, Craig DA, Gerald CP, Branchek TA. Swanson CJ, et al. Among authors: wolinsky td. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94. doi: 10.1073/pnas.0508970102. Epub 2005 Nov 15. Proc Natl Acad Sci U S A. 2005. PMID: 16287967 Free PMC article.
19 results