title: Synthesis, Antibacterial and Antitubercular Activities of Some 5H-Thiazolo[3,2-a]pyrimidin-5-ones and Sulfonic Acid Derivatives.
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, (13)C-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.
authors.affiliation: College of Basic Science, Liaoning Medical University, Jinzhou 121001, China. Caidong0804@163.com.
authors.forename: Dong
authors.initials: D
authors.lastname: Cai
authors.affiliation: School of Chemical and Environmental Engineering, Liaoning University of Technology, Jinzhou 121001, China. Bridge1026@163.com.
authors.forename: Zhi-Hua
authors.initials: ZH
authors.lastname: Zhang
authors.affiliation: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China. gzweishengwu@126.com.
authors.forename: Yu
authors.initials: Y
authors.lastname: Chen
authors.affiliation: College of Pharmacy, Harbin University of Commerce Harbin, Harbin 150076, China. yanxinjia@yeah.net.
authors.forename: Xin-Jia
authors.initials: XJ
authors.lastname: Yan
authors.affiliation: College of Basic Science, Liaoning Medical University, Jinzhou 121001, China. zouliangjing@yeah.net.
authors.forename: Liang-Jing
authors.initials: LJ
authors.lastname: Zou
authors.affiliation: College of Basic Science, Liaoning Medical University, Jinzhou 121001, China. 18341653394@163.com.
authors.forename: Ya-Xin
authors.initials: YX
authors.lastname: Wang
authors.affiliation: College of Basic Science, Liaoning Medical University, Jinzhou 121001, China. araqi1128@163.com.
authors.forename: Xue-Qi
authors.initials: XQ
authors.lastname: Liu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D066244:Proton Magnetic Resonance Spectroscopy; D013055:Spectrophotometry, Infrared; D013451:Sulfonic Acids / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D013451:Sulfonic Acids
keywords: antibacterial; antitubercular; sulfonation; thiazolo[3,2-a]pyrimidine