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Page 1
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
Rowbottom MW, Vickers TD, Dyck B, Grey J, Tamiya J, Zhang M, Kiankarimi M, Wu D, Dwight W, Wade WS, Schwarz D, Heise CE, Madan A, Fisher A, Petroski R, Goodfellow VS. Rowbottom MW, et al. Among authors: wade ws. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4450-7. doi: 10.1016/j.bmcl.2006.06.045. Epub 2006 Jun 30. Bioorg Med Chem Lett. 2006. PMID: 16814542
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.
Hudson S, Kiankarimi M, Rowbottom MW, Vickers TD, Wu D, Pontillo J, Ching B, Dwight W, Goodfellow VS, Schwarz D, Heise CE, Madan A, Wen J, Ban W, Wang H, Wade WS. Hudson S, et al. Among authors: wade ws. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4922-30. doi: 10.1016/j.bmcl.2006.06.049. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824755
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. Chen C, et al. J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454. J Med Chem. 2008. PMID: 19006286
23 results