1. Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
- Author
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Zhang, Tian-Yi, Zheng, Chang-Ji, Wu, Jie, Sun, Liang-Peng, and Piao, Hu-Ri
- Subjects
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ANTIBACTERIAL agents , *GRAM-positive bacteria , *GRAM-negative bacteria , *OXAZOLIDINONES , *IN vitro studies , *PYRAZOLES - Abstract
Graphical abstract Three novel series of dihydrotriazine derivatives were designed, synthesized, and evaluated for their antibacterial and antifungal activity. Abstract Three novel series of dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties were designed, synthesized and evaluated in terms of their antibacterial and antifungal activities. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains (including multidrug-resistant clinical isolates) and Gram-negative bacterial strains with minimum inhibitory concentration values in the range of 1–64 µg/mL. Compounds 4b and 4c presented the most potent inhibitory activity against Gram-positive bacteria (S. aureus 4220, MRSA 3167, QRSA 3519) and Gram-negative bacteria (E. coli 1924), with minimum inhibitory concentration values of 1 or 2 µg/mL. Compared with previous studies, these compounds exhibited a broad spectrum of inhibitory activity. The cytotoxic activity of the compounds 4a , 4b , 4c and 11n were assessed in L02 cells. In vitro enzyme study implied that compound 4c exerted its antibacterial activity through DHFR inhibition. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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