Design, synthesis, and evaluation of 5-sulfamoyl benzimidazole derivatives as novel angiotensin II receptor antagonists.
Design, synthesis, and evaluation of 5-sulfamoyl benzimidazole derivatives as novel angiotensin II receptor antagonists.
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DOI：
10.1016/j.bmc.2008.10.056
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发表时间：
2008-12-15
影响因子：
3.5
通讯作者：
Singh, Manjeet
中科院分区：
文献类型：
--
作者：
Kaur, Navneet;Kaur, Amardeep;Bansal, Yogita;Shah, Dhvanit I.;Bansal, Gulshan;Singh, Manjeet
设计并合成了一系列5-烷基氨磺酰基苯并咪唑类血管紧张素II受体拮抗剂。已评价了化合物的体外血管紧张素II拮抗作用和对离体大鼠主动脉环和醋酸脱氧可的松诱导的高血压大鼠的体内抗高血压活性。发现活性与烷基的大小有关。最大的活性是观察到一个紧凑和庞大的烷基，如叔丁基和环己基。化合物4g和4 h在体外和体内均显示出良好的活性。在构效关系的基础上提出了一个受体结合模型。
A series of 5-alkylsulfamoyl benzimidazole derivatives have been designed and synthesized as novel angiotensin II (Ang II) receptor antagonists. The compounds have been evaluated for in vitro Ang II antagonism and for in vivo antihypertensive activity on isolated rat aortic ring and desoxycortisone acetate induced hypertensive rats, respectively. The activity is found related to size of alkyl group. The maximum activity is observed with a compact and bulky alkyl group like tert-butyl and cyclohexyl. The compounds 4g and 4h have shown promising both in vitro and in vivo activities. A receptor binding model is also proposed on the basis on the basis of structure–activity relationship in this study.
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影响因子：
7.3
作者：
Berellini, G;Cruciani, G;Mannhold, R
通讯作者：
Mannhold, R
影响因子：
7.3
作者：
ASHTON, WT;CANTONE, CL;SIEGL, PKS
通讯作者：
SIEGL, PKS
影响因子：
7.3
作者：
KUBO, K;KOHARA, Y;NAKA, T
通讯作者：
NAKA, T
影响因子：
2.7
作者：
Bali, A;Bansal, Y;Singh, M
通讯作者：
Singh, M
DOI：
10.1111/j.1476-5381.1947.tb00336.x
发表时间：
1947-01-01
期刊：
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY
影响因子：
--
作者：
SCHILD, HO
通讯作者：
SCHILD, HO