Synthesis of New 2-Thio-[1,2,4]triazolo[1,5-c]quinazoline Derivatives and Its Antimicrobial Activity

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概要

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• A series of novel ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acids 2a—d and esters 3a—l were synthesized and evaluated for antimicrobial activity. Alkylation of potassium 2-thio-[1,2,4]triazolo[1,5-c]quinazoline 1 with halogenocarboxylic acids and its esters proceeded S-regioselectively. During acid catalyzed esterification of 2a—c, degradation of the pyrimidine ring was observed. The structures of the compounds were elucidated by FT-IR, 1H- and 13C-NMR, electron impact mass spectra (EI-MS) and LC-MS spectral data. Antimicrobial and antifungal activity of synthesized compounds was tested against Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger, Mycobacterium luteum, Candida albicans and Candida tenuis. Acids 2a and 2c exhibited significant activity against C. albicans, which was additionally confirmed by the bioluminescence inhibition test and interrelated with their lipophilicity.

• 公益社団法人　日本薬学会の論文

著者

• Antipenko Lyudmila

  Department of Pharmaceutical Chemistry, Zaporozhye State Medical University

• Karpenko Alexander

  Department of Pharmaceutical Chemistry, Zaporozhye State Medical University

• Kovalenko Sergey

  Department of Pharmaceutical Chemistry, Zaporozhye State Medical University

• Katsev Andrew

  Department of Pharmacy, Crimean State Medical University

• Komarovska-Porokhnyavets Elena

  Department of Technology of Biological Active Substances, Pharmacy and Biotechnology, National Unive

• Novikov Vladimir

  Department of Technology of Biological Active Substances, Pharmacy and Biotechnology, National Unive

• Chekotilo Aleksey

  Enamine Ltd.

関連論文

• Synthesis of New 2-Thio-[1,2,4]triazolo[1,5-c]quinazoline Derivatives and Its Antimicrobial Activity

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