Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

Back

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, Chuntao Zhang.

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

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 7
ISSUE: 6
Year: 2010
Page: [415 - 420]
Pages: 6
DOI: 10.2174/157018010791306560
Price: $58