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Synthesis and antimycobacterial activity of N′-[( E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives
Ist Teil von
European journal of medicinal chemistry, 2009-12, Vol.44 (12), p.4954-4959
Ort / Verlag
Kidlington: Elsevier Masson SAS
Erscheinungsjahr
2009
Quelle
MEDLINE
Beschreibungen/Notizen
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.
[Display omitted] A series of twenty-six pyrazine derivatives have been synthesized and evaluated against
M. tuberculosis. Compounds
6,
23,
27 and
28 exhibited a significant activity (50–100
μg/mL).