Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity | ||
| Bulletin of Pharmaceutical Sciences Assiut University | ||
| Article 3, Volume 22, Issue 1, June 1999, Pages 35-45 PDF (331.29 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/bfsa.1999.65970 | ||
| Author | ||
| Hoda Y. Hassan | ||
| Department of Pharmaceutical, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt | ||
| Abstract | ||
| Two series of nitropyridine derivs. bearing 2-thiazolyl hydrazines were synthesized and evaluated for their monoamine oxidase (MAO) inhibitory activity by in vitro tests to assay their effect on rat liver mitochondria by a kynuramine fluorimetric assay. The two key intermediates, 6-methyl-5-nitropyridine-2-carboxaldehyde thiosemicarbazone (I) and 1-(6-methyl-5-nitropicolinoyl)thiosemicarbazide (II), were prepd. by conventional methods. The target compds., N-(6-methyl-5-nitropyridin-2-ylmethylidene)-N'-(4-substituted thiazol-2-yl)hydrazines III (R = Me, Ph, 4-BrC6H4, 4-ClC6H4, 4-MeOC6H4, 4-O2NC6H4, X = CH:NNH) and 6-methyl-5-nitropyridine-2-carboxylic acid N'-(4-substituted thiazol-2-yl)hydrazides III (R = Me, Ph, 4-BrC6H4, 4-ClC6H4, 4-MeOC6H4, X = CONHNH), were prepd. by condensation of I or II with the appropriate α-halogeno-ketone, chloroacetone or phenacyl bromides. All the assayed compd. posses in vitro monoamine oxidase inhibitory activity at a concn. of 0.33 - 1.66 x 105 M. | ||
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