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65970

Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity

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Last updated: 04 Jan 2025

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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.

DOI

10.21608/bfsa.1999.65970

Authors

First Name

Hoda

Last Name

Hassan

MiddleName

Y.

Affiliation

Department of Pharmaceutical, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

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Volume

22

Article Issue

1

Related Issue

9968

Issue Date

1999-06-01

Receive Date

1998-09-22

Publish Date

1999-06-30

Page Start

35

Page End

45

Print ISSN

1110-0052

Online ISSN

3009-7703

Link

https://bpsa.journals.ekb.eg/article_65970.html

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https://bpsa.journals.ekb.eg/service?article_code=65970

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3

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Original Article

Type Code

1,096

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

https://bpsa.journals.ekb.eg/

MainTitle

Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity

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Article

Created At

22 Jan 2023