5-(Pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists
摘要:
A new series of 5-(pyridinon-1-yl)indazoles with MCH-1 antagonist activity were synthesized. Potential cardiovascular risk for these compounds was assessed based upon their interaction with the hERG potassium channel in a mini-patch clamp assay. Selected compounds were studied in a 5-day diet-induced obese mouse model to evaluate their potential use as weight loss agents. Structural modification of the 5-(pyridinon-1-yl) indazoles to give 5-(furopyridinon-5-yl) indazoles provided compounds with enhanced pharmacokinetic properties and improved efficacy. (C) 2010 Elsevier Ltd. All rights reserved.
Synthesis, Characterization, and Structures of Tetrakis(2-Pyridyl)Tin Compounds
摘要:
Reactions of 2-bromopyridine and 2-bromo-6-methylpyridine with n-BuLi and tin tetrachloride afforded Sn(2-py)(4) (1a) and Sn(6-Me-2-py)(4) (1b), respectively. The identities of the two compounds were unambiguously proved by microanalyses, NMR (H-1, C-13, Sn-119) spetroscopy, and single-crystal X-ray diffraction studies.
5-(Pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists
作者:Matthew D. Surman、Emily E. Freeman、James F. Grabowski、Mark Hadden、Alan J. Henderson、Guowei Jiang、Xiaowu (May) Jiang、Michele Luche、Yuri Khmelnitsky、Steven Vickers、Jean Viggers、Sharon Cheetham、Peter R. Guzzo
DOI:10.1016/j.bmcl.2010.09.039
日期:2010.12
A new series of 5-(pyridinon-1-yl)indazoles with MCH-1 antagonist activity were synthesized. Potential cardiovascular risk for these compounds was assessed based upon their interaction with the hERG potassium channel in a mini-patch clamp assay. Selected compounds were studied in a 5-day diet-induced obese mouse model to evaluate their potential use as weight loss agents. Structural modification of the 5-(pyridinon-1-yl) indazoles to give 5-(furopyridinon-5-yl) indazoles provided compounds with enhanced pharmacokinetic properties and improved efficacy. (C) 2010 Elsevier Ltd. All rights reserved.
Synthesis, Characterization, and Structures of Tetrakis(2-Pyridyl)Tin Compounds
作者:Martin Bette、Dirk Steinborn
DOI:10.1080/10426507.2012.702823
日期:2012.11.1
Reactions of 2-bromopyridine and 2-bromo-6-methylpyridine with n-BuLi and tin tetrachloride afforded Sn(2-py)(4) (1a) and Sn(6-Me-2-py)(4) (1b), respectively. The identities of the two compounds were unambiguously proved by microanalyses, NMR (H-1, C-13, Sn-119) spetroscopy, and single-crystal X-ray diffraction studies.