Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity
Hassan, H. (1999). Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity. EKB Journal Management System, 22(1), 35-45. doi: 10.21608/bfsa.1999.65970
Hoda Y. Hassan. "Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity". EKB Journal Management System, 22, 1, 1999, 35-45. doi: 10.21608/bfsa.1999.65970
Hassan, H. (1999). 'Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity', EKB Journal Management System, 22(1), pp. 35-45. doi: 10.21608/bfsa.1999.65970
Hassan, H. Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity. EKB Journal Management System, 1999; 22(1): 35-45. doi: 10.21608/bfsa.1999.65970

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, Page 35-45  XML PDF (331.29 K)
Document Type: Original Article
DOI: 10.21608/bfsa.1999.65970
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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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