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Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
Aminopyrazinoic acid esters as potential antimycobacterial drugs
Martin Doležal1, Jana Vobicková, Barbora Servusová
1Charles University in Prague, Faculty of Pharmacy, Department of Heyrowského, Czech Republic. martin.dolezal@faf.cuni.cz
Abstract:
A series of esters of the 3-aminopyrazine-2-carboxylic acid as potential antimycobacterial drugs was synthesized. A CEM Discover microwave reactor with an autosampler Explorer 24 which served to accelerate the reaction was used for synthesis. The prepared products were characterized by IR, 1H NMR, 13C NMR spectra, elementary analysis and melting points. Log P and ClogP values were calculated. Final products were evaluated in vitro for their antimycobacterial activity. The most active compound was hexyl 3-aminopyrazine-2-carboxylate (7), whose antimycobacterial activity (MIC) against M. tuberculosis H37Rv was 6.25 μg/mL.
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