Background: Oxadiazole derivatives are the biologically active heterocyclic compounds.
Thus, we synthesized a series of Mannich bases, 3-(arylaminomethyl)-5-(pyridin-
4-yl)-1,3,4-oxadiazole-(3H)-thi-2-one derivatives(3a-3g) were synthesized from Isoniazid [INH
(1)], a first line antimycobacterial drug, and these compounds were evaluated as antimycobacterial
Methods: The INH was reacted with potassium hydroxide and carbon disulfide to give 5-(pyridin-
4-yl)-1,3,4-oxadiazole-2(3H)-thione (2), followed by reacting compound 2 with appropriate aromatic
amines in the presence of formaldehyde to obtain desired compounds (3a-3g). The structures
of these compounds have been established by IR, 1H-NMR, Mass spectral and elemental analysis.
These synthesized compounds (3a-3g) were evaluated for their antimycobacterial activity against
M. tuberculosis H37Rv strain.
Results: All the synthesized compounds (3a-3g) exhibited antimycobacterial activity and were
compared to reference drugs Streptomycin (MIC value of 6.25μg/mL), INH (MIC value of
3.125μg/mL) and pyrazinamide (MIC value of 3.125μg/mL). Compounds 3c and 3e exhibited the
most promising antimycobacterial activity.
Conclusion: All the title compounds were synthesized and exhibited promising antimycobacterial
activity against M. tuberculosis H37Rv strain.