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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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 and Emad M. El-Telbani

Volume 13, Issue 9, 2016

Page: [921 - 931] Pages: 11

DOI: 10.2174/1570180813666160712234454

Price: $65

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).

Graphical Abstract


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