Novel pyrazolopiperazinone-and pyrrolopiperazinone-based MCH-R1 antagonists

…, J Méndez-Andino, AO Colson, XE Hu, JA Wos…

Index: Meyers, Kenneth M.; Mendez-Andino, Jose; Colson, Anny-Odile; Hu, X. Eric; Wos, John A.; Mitchell, Maria C.; Hodge, Karen; Howard, Jeremy; Paris, Jennifer L.; Dowty, Martin E.; Obringer, Cindy M.; Reizes, Ofer Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 3 p. 657 - 661

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Citation Number: 7

Abstract

... MCH-R1 in vitro activity for compounds 2a–f 9 and 10. Compound, R, X, Y, MCH-R1 Binding K i (nM) 10, 5HT 2C K i (μM). 2a, H, 3-F, Piperidyl, 22, >100. ... Through modification of the amide linker between the 4-fluorophenyl and the pyrrole rings in the pyrrolopiperazinone series, potency similar to that of pyrazolopiperazinones was achieved. ... M. Nishiguchi, T. Funakoshi, S. Chki, G. Semple, T.-A. Tran, B. Kramer, D. Hsu, M. Casper, B. Thomsen, Y. Sekiguchi; Bioorg ...