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Design,Synthesis, and Biological Evaluation of 3,5‐Disubstituted 2‐Pyrazineamide Derivatives as Antitubercular Agents
Authors:Nagaraja Reddy Gangarapu  A Ranganatham  Eeda Koti Reddy  H D Surendra  Ayyiliath M Sajith  Shivaraj Yellappa  Kothapalli Bannoth Chandrasekhar
Abstract: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.
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