학술논문

Substituted 1,3,5-Triazine Heterocycles: Synthesis and Antibacterial Activity.
Document Type
Article
Source
Pharmaceutical Chemistry Journal. Jan2024, Vol. 57 Issue 10, p1580-1585. 6p.
Subject
*TRIAZINE derivatives
*ANTIBACTERIAL agents
*DNA topoisomerase II
*ANTIMICROBIAL stewardship
*HETEROCYCLIC compounds
*DRUG standards
Language
ISSN
0091-150X
Abstract
Research and development of new antibacterial agents are desperately needed in modern medicine, particularly ones that can effectively combat multi-resistant bacteria. Herein, we report the synthesis of a new series of substituted 4-phenylthiazolyl-1,3,5-triazine derivatives and their physicochemical characterization using IR, mass, and 1H-NMR spectroscopy. Among the synthesized derivatives examined for antibacterial activity, one compound 6-chloro-N-(4-dimethylamino-phenyl)-N′-[4-(4-methoxy-phenyl)-thiazol-2-yl]-[1,3,5]-triazine-2,4-di-amine (SK4) demonstrated encouraging inhibition of both Gram-positive and Gram-negative bacteria compared with the standard drug ofloxacin. Another compound 4-(4,6-dichloro-1,3,5-triazine-2-yl)amino-benzoic acid (SK1) also exhibited significant antimicrobial activity against S. aureus. Apotential drug target, DNA gyrase, was found to be the most suitable for these molecules using molecular docking. Identified new hits are crucial for both antimicrobial stewardship and the prevention of antimicrobial resistance in the future. [ABSTRACT FROM AUTHOR]