- Synthesis andanti-mycobacterial evaluation of some pyrazine-2-carboxylic acid hydrazide derivatives
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A series of pyrazine-2-carboxylic acid hydrazide derivatives were synthesized and screened for their activity against Mycobacterium tuberculosis. The results show that pyrazine-2-carboxylic acid hydrazi-deehydrazone derivatives 3ael were less active than pyrazinamide. In contrast,the N 4-ethyl-N1-pyr-azinoyl-thiosemicarbazide 4 showed the highest activity against M. tuberculosis H37Rv (IC90 16.87 mg/mL). Details of the structureeactivity and structureecytotoxicity relationships are discussed.
- Abdel-Aziz, Mohamed,Bdel-Rahman, Hamdy M.A.
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experimental part
p. 3384 - 3388
(2010/08/13)
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- Synthesis and antimycobacterial activity of N′-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives
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The present article describes a series of twenty-six N′-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide (4-29), which were synthesized and evaluated for their cell viabilities in non infected and infected macrophages with Mycobacterium bovis Bacillus Calmette-Guerin (BCG). Afterwards, the non-cytotoxic compounds (4, 6, 8, 15, 21, 23, 24, 27 and 28) were assessed against Mycobacterium tuberculosis ATCC 27294 using the micro plate Alamar Blue assay (MABA) and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. The compounds 6, 23, 27 and 28 exhibited a significant activity (50-100 μg/mL) when compared with first line drugs such as pyrazinamide and were not cytotoxic in their respective MIC values.
- Vergara, Fatima M.F.,Lima, Camilo H. da S.,Henriques, Maria das Gracas M. de O.,Candea, Andre L.P.,Lourenco, Maria C.S.,Ferreira, Marcelle de L.,Kaiser, Carlos R.,de Souza, Marcus V.N.
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experimental part
p. 4954 - 4959
(2010/02/27)
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