Design and green synthesis of 2-(diarylalkyl)aminobenzothiazole derivatives and their dual activities as angiotensin converting enzyme inhibitors and calcium channel blockers

被引：27

作者：

Kalavagunta, Praveen Kumar ^{[1
]}

Bagul, Pankaj K. ^{[2
]}

Jallapally, Anvesh ^{[1
,2
]}

Kantevari, Srinivas ^{[1
]}

Banerjee, Sanjay K. ^{[2
]}

Ravirala, Narender ^{[1
]}

机构：

[1] Indian Inst Chem Technol, CSIR, Crop Protect Chem Div, Hyderabad 500007, Andhra Pradesh, India

[2] Indian Inst Chem Technol, CSIR, Med Chem & Pharmacol Div, Hyderabad 500007, Andhra Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 83卷

关键词：

ACE inhibitors; Calcium channel blockers; Green synthesis; 2-Aminobenzothiazole; Diarylalkylamine; Resistant hypertension; RILUZOLE; ANTAGONISTS; ACTIVATION;

D O I：

10.1016/j.ejmech.2014.06.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 2-(diarylalkyl)aminobenzothiazoles were designed based on commercial synthetic calcium channel blockers (CCBs) and angiotensin converting enzyme (ACE) inhibitors. Which are further modified based on the natural products which are angiotensin converting enzyme (ACE) inhibitors. Completely green protocol was developed for their synthesis. As they are initially designed based on CCBs, they were screened for their ACE inhibition property believing that almost all the compounds will be CCBs. Out of 42 compounds two lead molecules were identified as ACE inhibitors, which were further screened for CCB. As expected both were identified as CCBs with different selectivity over ACE inhibition. Their selectivity over ACE and CCB can be used to treat resistant hypertension. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：344 / 354

页数：11

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