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

Molecules

Dong Cai²  Zhi-Hua Zhang³  Yu Chen¹  Xin-Jia Yan⁴  Liang-Jing Zou²  Ya-Xin Wang²  Xue-Qi Liu² 

[1] School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China; E-Mail:;College of Basic Science, Liaoning Medical University, Jinzhou 121001, China; E-Mails:;School of Chemical and Environmental Engineering, Liaoning University of Technology, Jinzhou 121001, China; E-Mail:;College of Pharmacy, Harbin University of Commerce Harbin, Harbin 150076, China; E-Mail:

关键词: thiazolo[3;    2-a]pyrimidine;    sulfonation;    antibacterial;    antitubercular;   

DOI  :  10.3390/molecules200916419

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
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