Synthesis and biological activities of triazole derivatives as inhibitors of InhA and antituberculosis agents

Crystal structure of 2-(5-(4-fluorophenyl)-3-p-tolyl-4,5-dihydro-1H-pyrazol-1-yl)-4-(5-methyl-1-p-tolyl-1H-1,2,3-triazol-4-yl)thiazole, C29H25FN6S

“…Various heterocycles containing triazole ring . have been synthesized [2][3][4][5][6][7][8][9][10]. They show a variety of interesting biological activities and can be used as antimicrobial agents [2][3][4][5][6][7][8][9][10].…”

Synthesis and evaluation of β-hydroxytriazoles and related compounds as antitubercular agents

“…Finally, decreasing the quantity of reactants or lowering the temperature is detrimental to the yield, even after 20 h (entries 8,10). With this method in hand (entry 9), several β-alcohols were oxidized allowing the obtention of the corresponding α,β-diketotriazoles in good yields as shown in Table 1.…”

“…Among them, nine hydroxyl-triazoles were evaluated and particularly one compound bearing a n-butyl substituent at position 4 of the triazole ( Figure 1, middle) showed the best activity with a MIC of 25 µM. Our group also reported the synthesis of triazole derivatives and their evaluation as M.tb inhibitors [8][9][10][11]. Among them, several compounds showed interesting MIC values when tested against M.tb and M.tb antibioticresistant strains.…”

“…Among them, several compounds showed interesting MIC values when tested against M.tb and M.tb antibioticresistant strains. In continuation of our research on the synthesis of biologically active heterocycles against tuberculosis [8,[10][11][12], we wish to report the synthesis and the evaluation of a wide range of β-hydroxytriazole derivatives against M.tb H37Rv (Figure 1, right). This work also described the antitubercular activities of a new series of α,β-diketotriazoles and styryl triazoles synthesized conveniently from the corresponding β-hydroxytriazoles.…”

Mycobacterium tuberculosisenoyl-acyl carrier protein reductase inhibitors as potential antituberculotics: development in the past decade

“…The best results were achieved with class b (Figure 9) compound bearing a nonyl substituent (50), however, it showed only 58% inhibition at 50 mM concentration. Good antimycobacterial activities compared in relation to poor InhA inhibition suggest presence of another target distinct from InhA 35 .…”