Synthesis and Antimicrobial Evaluation of New Pyrazoline and Pyrazolinyl Thiazole Derivatives Bearing Tetrazolo[1,5-a]quinoline Moiety

Author(s): Ibrahim A. M. Radini, Rizk E. Khidre, Emad M. El-Telbani.

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 9 , 2016

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Graphical Abstract:


The reaction of 1-heteroaryl-3-(tetrazolo[1,5-a]quinolin-4-yl)prop-2-en-1-ones with hydrazine hydrate in either ethanol or acetic acid furnished pyrazoline and N-acetylpyrazoline, respectively. N-phenylpyrazolines and pyrazoline-N-carbothioamides were synthesized, in good yields, from reaction of chalcons with phenylhydrazine and thiosemicarbazide, respectively. On the other hand, a series of 2-pyrazolin-1-ylthiazoles have been synthesized via cyclization of pyrazoline-Ncarbothioamides with different -haloketones such as phenacyl bromides, 3-bromoacetylcoumarin, hydrazonoyl chlorides, and -chloroacetic acid. The structures of the newly synthesized compounds have been confirmed by spectral analyses also the in vitro antimicrobial activities were studied.

Keywords: Tetrazolo[1, 5-a]quinoline-4-carbaldehyde, chalcones, pyrazolines, pyrazolinylthiazoles, antimicrobial activity, structure-activity relationship (SAR).

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Article Details

Year: 2016
Page: [921 - 931]
Pages: 11
DOI: 10.2174/1570180813666160712234454
Price: $65

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