A series of thiazolidin-4-one (2a-h, 3a-h), azetidin-2-one (4a- h) and
1,3,4-oxadiazole (5a-h) derivatives of isoninicotinic acid hydrazide (INH)
were synthesized in order to obtain new compounds with potential
anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities.
The structures of the new compounds were supported by their IR, 1H-NMR and
mass spectral data. All compounds were evaluated for their anti-inflammatory
activity by the carrageenan-induced rat paw edema test method. Eleven of the
new compounds, out of 32, showed very good anti-inflammatory activity in the
carrageenan-induced rat paw edema test, with significant analgesic activity
in the tail immersion method together with negligible ulcerogenic action.
The compounds, which showed less ulcerogenic action, also showed reduced
malondialdehyde content (MDA), which is one of the by-products of lipid
peroxidation. The study showed that the compounds inhibited the induction of
gastric mucosal lesions and it can be suggested from the results that their
protective effects may be related to inhibition of lipid peroxidation in the
gastric mucosa.