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: Martin Juh ás Lucie Ku čerová Ond řej Horáček Ond řej Janďourek Vladim ír Kubíček Kl ára Konečná Radim Ku čera Pavel B árta Ji ří Janoušek Pavla Paterov á Ji ří Kuneš Martin Dole žal Jan Zitko Tags: Article Source Type: research
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