Catalyst free sequential one-pot reaction for the synthesis of 3-indole propanoates/propanoic acid/propanamides as antituberculosis agents

被引：10

作者：

Rajeev, Narasimhamurthy ^{[1
]}

Sharath Kumar, Kothanahally S. ^{[1
]}

Bommegowda, Yadaganahalli K. ^{[1
]}

Rangappa, Kanchugarakoppal S. ^{[2
]}

Sadashiva, Marilinganadoddi P. ^{[1
]}

机构：

[1] Univ Mysore, Dept Studies Chem, Mysuru 570006, India

[2] Univ Mysore, Inst Excellence, Mysuru 570006, India

来源：

JOURNAL OF THE CHINESE CHEMICAL SOCIETY | 2021年 / 68卷 / 01期

关键词：

indole; Meldrum' s acid; Michael addition; multicomponent and tuberculosis; ASYMMETRIC MICHAEL ADDITION; FRIEDEL-CRAFTS ALKYLATION; MELDRUMS ACID; EASY ACCESS; INDOLES; DERIVATIVES; APOPTOSIS; PYRIDINE; ALPHA; ENANTIOSELECTIVITY;

D O I：

10.1002/jccs.202000386

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A highly efficient catalyst free one pot four component synthesis of highly functionalized three-substituted indole derivatives has been reported. Thus, sequential catalyst free condensation of readily available aldehydes with Meldrum's acid followed by Michael addition of indole resulting three carbon component condensed product and concurrent decarboxylation by the nucleophilic attack of ethanol/water/amines affords three-indole propanoates/propanoic acid/propanamides in affordable yields. Further, synthesized compounds and standard drugs were evaluated against Mycobacterium tuberculosis H37Rv strain by Alamar blue assay method. Majority of the compounds exhibited the superior activity and specifically compound 4d has MIC 1.6 mu g/ml, which is better than the reference drugs used.

引用

页码：39 / 44

页数：6

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