Mechanochemical Synthesis and Biological Evaluation of Novel Isoniazid Derivatives with Potent Antitubercular Activity
AbstractA series of isoniazid derivatives bearing a phenolic or heteroaromatic coupled frame were obtained by mechanochemical means. Their pH stability and their structural (conformer/isomer) analysis were checked. The activity of prepared derivatives against Mycobacterium tuberculosis cell growth was evaluated. Some compounds such as phenolic hydrazine 1a and almost all heteroaromatic ones, especially 2, 5 and 7, are more active than isoniazid, and their activity against some M. tuberculosis MDR clinical isolates was determined. Compounds 1a and 7 present a selectivity index >1400 evaluated on MRC5 human fibroblast cells. The mechanism of action of selected hydrazones was demonstrated to block mycolic acid synthesis due to InhA inhibition inside the mycobacterial cell. View Full-Text
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Oliveira, P.F.M.; Guidetti, B.; Chamayou, A.; André-Barrès, C.; Madacki, J.; Korduláková, J.; Mori, G.; Orena, B.S.; Chiarelli, L.R.; Pasca, M.R.; Lherbet, C.; Carayon, C.; Massou, S.; Baron, M.; Baltas, M. Mechanochemical Synthesis and Biological Evaluation of Novel Isoniazid Derivatives with Potent Antitubercular Activity. Molecules 2017, 22, 1457.
Oliveira PFM, Guidetti B, Chamayou A, André-Barrès C, Madacki J, Korduláková J, Mori G, Orena BS, Chiarelli LR, Pasca MR, Lherbet C, Carayon C, Massou S, Baron M, Baltas M. Mechanochemical Synthesis and Biological Evaluation of Novel Isoniazid Derivatives with Potent Antitubercular Activity. Molecules. 2017; 22(9):1457.Chicago/Turabian Style
Oliveira, Paulo F.M.; Guidetti, Brigitte; Chamayou, Alain; André-Barrès, Christiane; Madacki, Jan; Korduláková, Jana; Mori, Giorgia; Orena, Beatrice S.; Chiarelli, Laurent R.; Pasca, Maria R.; Lherbet, Christian; Carayon, Chantal; Massou, Stéphane; Baron, Michel; Baltas, Michel. 2017. "Mechanochemical Synthesis and Biological Evaluation of Novel Isoniazid Derivatives with Potent Antitubercular Activity." Molecules 22, no. 9: 1457.
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