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Molecules 2015, 20(9), 16419-16434; doi:10.3390/molecules200916419

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

1
College of Basic Science, Liaoning Medical University, Jinzhou 121001, China
2
School of Chemical and Environmental Engineering, Liaoning University of Technology, Jinzhou 121001, China
3
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China
4
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)
View Full-Text   |   Download PDF [630 KB, uploaded 14 September 2015]   |  

Abstract

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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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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