Letters in Drug Design & Discovery

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


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.


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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Article Details

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