Molecules, Vol. 25, Pages 1518: N-Pyrazinoyl Substituted Amino Acids as Potential Antimycobacterial Agents —The Synthesis and Biological Evaluation of Enantiomers

Molecules, Vol. 25, Pages 1518: N-Pyrazinoyl Substituted Amino Acids as Potential Antimycobacterial Agents—The Synthesis and Biological Evaluation of Enantiomers Molecules doi: 10.3390/molecules25071518 Authors: Martin Juhás Lucie Kučerová Ondřej Horáček Ondřej Janďourek Vladimír Kubíček Klára Konečná Radim Kučera Pavel Bárta Jiří Janoušek Pavla Paterová Jiří Kuneš Martin Doležal Jan Zitko Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis (Mtb), each year causing millions of deaths. In this article, we present the synthesis and biological evaluations of new potential antimycobacterial compounds containing a fragment of the first-line antitubercular drug pyrazinamide (PZA), coupled with methyl or ethyl esters of selected amino acids. The antimicrobial activity was evaluated on a variety of (myco)bacterial strains, including Mtb H37Ra, M. smegmatis, M. aurum, Staphylococcus aureus, Pseudomonas aeruginosa, and fungal strains, including Candida albicans and Aspergillus flavus. Emphasis was placed on the comparison of enantiomer activities. None of the synthesized compounds showed any significant activity against fungal strains, and their antibacterial activities were also low, the best minimum inhibitory concentration (MIC) value was 31.25 µM. However, several compounds presented high activity against Mtb. Overall, higher activity was seen in derivatives containing ʟ-amino acids. Similarly, the a...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research