Bioorganic and Medicinal Chemistry Letters p. 1079 - 1084 (2019)
Update date:2022-08-05
Topics:
Zhang, Tian-Yi
Zheng, Chang-Ji
Wu, Jie
Sun, Liang-Peng
Piao, Hu-Ri
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.
View MoreShanghai Zhihua ChemTech Co., Ltd.
Contact:+86-13774313779
Address:Room 817 Suite B 3333 Shenjiang Road
Nanjing distinctions Medical Technology Co., Ltd.(expird)
Contact:+86-15996203785 13914714059
Address:nanjing,jiangsu , China
ShangHai Soyoung Biotechnology Inc
website:http://www.soyoungbio.com
Contact:+86-21-69893009
Address:shanghai
Contact:86-571-61063068
Address:LINAN
Luojiang Chenming Biological Products Co
Contact:+86 15000297032
Address:GROUP NO.4, HE SHENG VILLAGE, PANLONG TOWN,
Doi:10.1021/bc400306g
(2013)Doi:10.1021/ja00988a041
(1967)Doi:10.1016/S0040-4039(00)90753-6
(1967)Doi:10.1021/jo000235t
(2000)Doi:10.1039/jr9530002795
(1953)Doi:10.1016/S0040-4039(00)91691-5
(1992)