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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Design, Synthesis and Biological Evaluation of Benzopyran Derivatives as KATP Channel Openers

Author(s): Jinpei Zhou, Hai Qian, Huibin Zhang, Hui Gao, Wenlong Huang, Xiaoyun Zhu, Shuaijian Ni and Chuntao Zhang

Volume 7, Issue 6, 2010

Page: [415 - 420] Pages: 6

DOI: 10.2174/157018010791306560

Price: $65

Abstract

In order to complete the SAR and discover new potent and selective PCOs, some changes were made to the C-4 and C-2 substitutions of cromakalim. A series of 4 -amino acid substituted -2, 2-dialkylchromans structurally related to cromakalim were synthesized and evaluated, as ATP-sensitive potassium channel openers (8a-l). Preliminary biological tests suggested that these compounds exhibited potent to mild relaxation activity of the KCl-contracted rat aortic strips. Compounds 8b (IC50 =0.25μM), 8f (IC50 =6.44μM) and 8j (IC50 =8.65μM) exhibited commendable opening activity of potassium channels. In addition to anti-hypertension, these compounds can also be considered as lead candidates for the further development of myocardial antiischemic drugs.

Keywords: Anti-hypertension, KATP Channel Openers, Benzopyran derivatives, Synthesis


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