期刊：
LETTERS IN DRUG DESIGN & DISCOVERY,2010年7(6):415-420 ISSN：1570-1808
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.
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 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.
作者机构：
[李焕德; 王峰; 向大雄; 周志凌; 肖轶雯; 原海燕; 徐萍] Clinical Pharmacy Laboratory, Second Xiangya Hospital, Central South University, Changsha 410011, China;[周晋] Hunan Coll. Traditional Chinese M., Changsha 410007, China
通讯机构：
[Wang, F.] C;Clinical Pharmacy Laboratory, Second Xiangya Hospital, Central South University, China
