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

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成果类型:
期刊论文
作者:
Zhou, Jinpei;Qian, Hai;Zhang, Huibin*;Gao, Hui;Huang, Wenlong;...
通讯作者:
Zhang, Huibin
作者机构:
[Zhou, Jinpei] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China.
[Gao, Hui; Qian, Hai; Zhu, Xiaoyun; Ni, Shuaijian; Zhang, Huibin; Huang, Wenlong] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210009, Peoples R China.
[Zhang, Chuntao] Hunan Univ Tradit Chinese Med, Organ & Med Chem Teaching & Res Sect, Changsha 410208A, Peoples R China.
[Zhang, Huibin] China Pharmaceut Univ, Ctr Drug Discovery, 24 Tongjiaxiang, Nanjing 210009, Peoples R China.
通讯机构:
[Zhang, Huibin] C
China Pharmaceut Univ, Ctr Drug Discovery, 24 Tongjiaxiang, Nanjing 210009, Peoples R China.
语种:
英文
关键词:
Anti-hypertension;KATP Channel Openers;Benzopyran derivatives;Synthesis
期刊:
LETTERS IN DRUG DESIGN & DISCOVERY
ISSN:
1570-1808
年:
2010
卷:
7
期:
6
页码:
415-420
基金类别:
National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [30973638]
机构署名:
本校为其他机构
摘要:
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 ...

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