4.5 Article

Synthesis and Antimycobacterial Activity of a Novel Series of Isonicotinylhydrazide Derivatives

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ARCHIV DER PHARMAZIE
卷 342, 期 12, 页码 723-731

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.200900001

关键词

Antimycobacterial activity; Azetidinones; Isonicotinyl hydrazide; Mycobacterium tuberculosis; Thiazolidinones

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A novel series of 14 new isonicotinyl hydrazide derivatives 2a-g, 3a-g containing a 4-thiazolidinone / 2-azetidinone nucleus were synthesized by reacting N'-substituted arylidene / heteroarylidene isonicotinyl hydrazide la-g with thioglycollic acid in the presence of dry benzene and with chloroacetyl chloride in the presence of triethylamine, respectively. Structures of all newly synthesized compounds were characterized on the basis of elemental analyses and spectral data (IR and H-1-NMR). All the title compounds were tested for their in-vitro antimycobacterial activity against Mycobacterium tuberctilosis H(37)Rv using Alamar-Blue susceptibility test, and the activity is expressed as the minimum inhibitory concentration (MIC) in mu g/mL. Among the series, compounds 2b, 2g, 3b, and 3g displayed an encouraging antimycobacterial activity profile as compared to that of the reference drugs isoniazid / rifampicin.

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