期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 20, 页码 5554-5558出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.09.009
关键词
PDE4; type 4 phosphodiesterase; 1,8-naphthyridin-4-one-3-carboxamides; asthma; COPD; MK-0873
A SAR study of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides is described. Optimization of the series was based on in vitro potency against PDE4, inhibition of the LPS-induced production of TNF-alpha in human whole blood and minimizing affinity for the hERG potassium channel. From these studies, compounds 18 and 20 (MK-0873) were identified as optimized PDE4 inhibitors with good overall in vitro and in vivo profiles and selected as development candidates. (c) 2008 Elsevier Ltd. All rights reserved.
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