Synthesis, Antibacterial and Antitubercular Activities of Some 5H-Thiazolo3,2-apyrimidin-5-ones and Sulfonic Acid DerivativesReportar como inadecuado




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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

Abstract A series of 5H-thiazolo3,2-apyrimidin-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-thiazolo3,2-apyrimidin-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: thiazolo3,2-apyrimidine; sulfonation; antibacterial; antitubercular thiazolo3,2-apyrimidine; sulfonation; antibacterial; antitubercular





Autor: Dong Cai 1,* , Zhi-Hua Zhang 2, Yu Chen 3, Xin-Jia Yan 4, Liang-Jing Zou 1, Ya-Xin Wang 1 and Xue-Qi Liu 1

Fuente: http://mdpi.com/



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