Molecules (2019)
Update date:2022-09-26
Topics:
Liu, Lili
Shao, Liping
Li, Jing
Cui, Haifeng
Li, Bing
Zhou, Xuzheng
Lv, Pengyue
Zhang, Jiyu
To combat bacterial resistance, a series of new oxazolidinone-fluoroquinolone hybrids have been synthesized and characterized. All synthetic hybrids were preliminarily evaluated for their in vitro antibacterial activities against 6 standard strains and 3 clinical isolates. The majority of hybrids displayed excellent activities against Gram-positive bacteria, but limited activities against Gram-negative bacteria. Hybrids OBP-4 and OBP-5 were found to be the most promising compounds. Further, in vitro antibacterial activities, mode of action and acute toxicity in mice of hybrids OBP-4 and OBP-5 were investigated. Hybrids OBP-4 and OBP-5 exhibited potent activities against Gram-positive bacteria, including drug-resistant strains. Correspondingly, studies on the mode of action of hybrids OBP-4 and OBP-5 indicated a strong inhibitory activity on protein synthesis by binding the active site of 50S subunit, but a weak inhibitory action on DNA synthesis. In addition, LD50 values of hybrids OBP-4 and OBP-5 in the acute oral toxicity were larger than 2000 mg/kg, suggesting a good safety profile.
View MoreContact:+86-519-86623222
Address:29F/D, 99 Yanling West Road, Changzhou, Jiangsu, China
Suzhou Sibian Chemical Technology Co., Ltd
website:http://www.sibianpharm.com
Contact:+8618169181984,+8618013186906
Address:Room1404,BuildingA,Jiabao Square No.323 Baodai East Road,Wuzhong District,Suzhou Jiangsu China (215128)
Kunshan Yalong Trading Co,.Ltd
Contact:86-512-57621185
Address:805-807 Room Hongqiao Mansion ,1088 West Qianjin Road, Kunshan, Jiangsu,China
Jinan Baozhao Pharmaceutical Co., Ltd
Contact:0086-531-86397156 82371858 82371868
Address:Huaneng Road, Jinan, Shandong ,China
Shanghai Yurui Biotechnology(Anyang) Pharmaceutical Co., Ltd
Contact:+86-0372-3662335 +86-0372-3661988
Address:hanling industrial park anyang
Doi:10.1002/jlcr.3637
(2018)Doi:10.1016/S0022-328X(00)91810-2
(1977)Doi:10.1016/j.jorganchem.2006.09.031
(2006)Doi:10.1016/0022-5088(84)90226-1
(1984)Doi:10.1021/jm00342a044
(1963)Doi:10.1016/j.tetlet.2006.11.045
(2007)