National Repository of Grey Literature 3 records found  Search took 0.01 seconds. 
Synthesis and evaluation of potential antimycobacterial agents based on hydrazine derivatives
Koklarová, Apolena ; Krátký, Martin (advisor) ; Vinšová, Jarmila (referee)
Based on research in past years, we have synthetized two similar series of compounds with potential antimycobacterial activity. First series based on isoniazid are (E)-4-[(2- isonicotinoylhydrazineylidene)methyl]-N-phenylbenzamides with great activity (MIC for Mtb. of 0.03-0.125 μM) with few derivatives with moderate activity on nontuberculous mycobacterium M. kansasii (MIC of 2-4 μM). In second series pyridin-4-yl moiety has been exchanged for 3,5-dinitrophenyl, which has shown to be highly effective antimycobacterial scaffold in recent years, therefore derivatives of (E)-4-{[2-(3,5- dinitrobenzoyl)hydrazineylidene]methyl}-N-phenylbenzamide have been prepared. These molecules have shown moderate activity against drug-susceptible Mtb. (MIC of 2-32 μM), and only 4-chloro derivative has surprisingly high activity against non-tuberculous M. avium (MIC of 16-32 μM). Four molecules from the second series even exhibit some activity against MDR- TB and XDR-TB strains.
Synthesis and evaluation of potential antimycobacterial agents based on hydrazine derivatives
Koklarová, Apolena ; Krátký, Martin (advisor) ; Vinšová, Jarmila (referee)
Based on research in past years, we have synthetized two similar series of compounds with potential antimycobacterial activity. First series based on isoniazid are (E)-4-[(2- isonicotinoylhydrazineylidene)methyl]-N-phenylbenzamides with great activity (MIC for Mtb. of 0.03-0.125 μM) with few derivatives with moderate activity on nontuberculous mycobacterium M. kansasii (MIC of 2-4 μM). In second series pyridin-4-yl moiety has been exchanged for 3,5-dinitrophenyl, which has shown to be highly effective antimycobacterial scaffold in recent years, therefore derivatives of (E)-4-{[2-(3,5- dinitrobenzoyl)hydrazineylidene]methyl}-N-phenylbenzamide have been prepared. These molecules have shown moderate activity against drug-susceptible Mtb. (MIC of 2-32 μM), and only 4-chloro derivative has surprisingly high activity against non-tuberculous M. avium (MIC of 16-32 μM). Four molecules from the second series even exhibit some activity against MDR- TB and XDR-TB strains.

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