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

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

Volume: 7 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Zhou Jinpei, Qian Hai, Zhang Huibin, Gao Hui, Huang Wenlong, Zhu Xiaoyun, Ni Shuaijian and Zhang Chuntao, Design, Synthesis and Biological Evaluation of Benzopyran Derivatives as KATP Channel Openers, Letters in Drug Design & Discovery 2010; 7 (6) . https://dx.doi.org/10.2174/157018010791306560