Design, Synthesis, and Biological Evaluation of 3,5‐Disubstituted 2‐Pyrazineamide Derivatives as Antitubercular Agents

A novel series of 3,5‐disubstituted‐2‐pyrazineamide derivatives (5a–5o) were synthesized and studied for their potential as antitubercular agents. Among them, the compounds 5a, 5g, and 5m showed the good minimal inhibitory concentration of 20, 25, and 25 μg/mL, respectively. The compound 5a displaye...

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Bibliographic Details
Published in:Journal of heterocyclic chemistry 2019-03, Vol.56 (3), p.1117-1126
Main Authors: Gangarapu, Nagaraja Reddy, Ranganatham, A., Reddy, Eeda Koti, Surendra, H. D., Sajith, Ayyiliath M., Yellappa, Shivaraj, Chandrasekhar, Kothapalli Bannoth
Format: Article
Language:English
Subjects:
Derivatives
Docking
Enzymes
Substrates
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Summary:A novel series of 3,5‐disubstituted‐2‐pyrazineamide derivatives (5a–5o) were synthesized and studied for their potential as antitubercular agents. Among them, the compounds 5a, 5g, and 5m showed the good minimal inhibitory concentration of 20, 25, and 25 μg/mL, respectively. The compound 5a displayed excellent minimum inhibitory concentration of 10 μg/mL and is four times more potent compared with the standard drug, rifampicin concentration. In silico docking studies revealed that the compounds 5a and 5c can bind strongly in the active site of 2FUM enzyme and prevent enzyme–substrate interactions. In addition, in silico docking studies were calculated, and based on the data obtained, compound 5a displayed excellent drug‐like properties.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.3461