Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues

被引：31

作者：

Ahsan, Mohamed Jawed ^{[1
,2
]}

Samy, Jeyabalan Govinda ^{[1
]}

Dutt, Kunduri Rajeswar ^{[2
]}

Agrawal, Uttam K. ^{[1
]}

Yadav, Bhawani Shankar ^{[1
]}

Vyas, Swati ^{[1
]}

Kaur, Ravinder ^{[1
]}

Yadav, Garima ^{[1
]}

机构：

[1] Alwar Pharm Coll, Dept Med Chem, New Drug Discovery Res, Alwar 301030, Rajasthan, India

[2] Natl Inst Med Sci Univ, Dept Pharmaceut Sci, Jaipur 303121, Rajasthan, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 15期

关键词：

Pyrazolines; Antitubercular agents; ANTITUBERCULAR ACTIVITY; DERIVATIVES; DRUGS;

D O I：

10.1016/j.bmcl.2011.06.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the present investigation, a series of 3-substituted-N-aryl-6,7-dimethoxy-3a, 4-dihydro-3-Hindeno[1,2-c]pyrazole-2-carboxamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed moderate to high inhibitory activities against Mycobacterium tuberculosis H(37)Rv and INH resistant M. tuberculosis. The compound N,3-bis(4-fluorophenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c] pyrazole-2-carboxamide (4c) was found to be the most promising compound active against M. tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentration 0.78 mu M. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：4451 / 4453

页数：3

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