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.