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Molecules 2015, 20(9), 16419-16434;

Synthesis, Antibacterial and Antitubercular Activities of Some 5H-Thiazolo[3,2-a]pyrimidin-5-ones and Sulfonic Acid Derivatives

College of Basic Science, Liaoning Medical University, Jinzhou 121001, China
School of Chemical and Environmental Engineering, Liaoning University of Technology, Jinzhou 121001, China
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China
College of Pharmacy, Harbin University of Commerce Harbin, Harbin 150076, China
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 4 August 2015 / Revised: 1 September 2015 / Accepted: 3 September 2015 / Published: 10 September 2015
(This article belongs to the Section Medicinal Chemistry)
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A series of 5H-thiazolo[3,2-a]pyrimidin-5-ones were synthesized by the cyclization reactions of S-alkylated derivatives in concentrated H2SO4. Upon treatment of S-alkylated derivatives at different temperatures, intramolecular cyclization to 7-(substituted phenylamino)-5H-thiazolo[3,2-a]pyrimidin-5-ones or sulfonation of cyclized products to sulfonic acid derivatives occurred. The structures of the target compounds were confirmed by IR, 1H-NMR, 13C-NMR and HRMS studies. The compounds were evaluated for their preliminary in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria and screened for antitubercular activity against Mycobacterium tuberculosis by the broth dilution assay method. Some compounds showed good antibacterial and antitubercular activities. View Full-Text
Keywords: thiazolo[3,2-a]pyrimidine; sulfonation; antibacterial; antitubercular thiazolo[3,2-a]pyrimidine; sulfonation; antibacterial; antitubercular

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Cai, D.; Zhang, Z.-H.; Chen, Y.; Yan, X.-J.; Zou, L.-J.; Wang, Y.-X.; Liu, X.-Q. Synthesis, Antibacterial and Antitubercular Activities of Some 5H-Thiazolo[3,2-a]pyrimidin-5-ones and Sulfonic Acid Derivatives. Molecules 2015, 20, 16419-16434.

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