Bioorganic and Medicinal Chemistry (2020)
Update date:2022-08-22
Topics:
Vigliotta, Giovanni
Giordano, Deborah
Verdino, Anna
Caputo, Ivana
Martucciello, Stefania
Soriente, Annunziata
Marabotti, Anna
De Rosa, Margherita
Antimicrobial resistance is spreading massively in the world and is becoming one of the main health threats of the 21st century. One of the possible strategies to overcome this problem is to modify the known classes of antibiotics in a rational way, with the aim of tuning their efficacy. In this paper, we present the synthesis and the evaluation of the biological activity of a series of two β-lactam bearing cephalosporin derivatives, in which an additional isolated azetidinone ring, bearing different substituents, is joined to the classical cephalosporanic nucleus by a chain of variable length. A computational approach has been also applied in order to predict the molecular interactions between some representative derivatives and selected penicillin-binding proteins, the natural targets of β-lactam antibiotics. All these derivatives are active against Gram-positive bacteria, with MIC100 comparable or even better than that of the reference antibiotic ceftriaxone, and show no or very low cytotoxic activity on different cell lines. Overall, these molecules appear to be able to exert their activity in particular against microorganisms belonging to some of the species more involved in the development of multidrug resistance.
View MoreQingdao S. H. Huanyu Imp. & Exp. Co., Ltd.
Contact:86-532-88250866
Address:Room 615, World Trade Centre Building B, Hongkong Middle Roda 6#, Qingdao, Shandong, China
Guangzhou PI & PI Biotech Inc. Ltd.
Contact:+86-20-81716320
Address:Suite 501,198 Kaiyuan Ave.,Science City, Guangzhou,China
jiangsu hualin chemical co.,ltd.
Contact:86-25-87787402
Address:jaingsu,china
Ceresking Ecology & Technology co.,ltd
Contact:86 22 66218397
Address:Room 1613, Zheshang Mansion, No. 1988, Yingbin Avenue, Binhai New District, Tianjin,China.
Fuxin Jintelai Fluorin Chemical Co., Ltd.
Contact:+86-0418-8229599
Address:, 7th Huagong Road, Fluorine industry development zone (Yimatu Town,Fumeng County),Fuxin City, Liaoning Province, China
Doi:10.1016/0040-4039(94)88181-2
(1994)Doi:10.1039/c39800001169
(1980)Doi:10.1021/jo01344a502
(1966)Doi:10.1055/s-0037-1610909
(2019)Doi:10.1016/j.bmc.2016.06.006
(2016)Doi:10.1039/c9ob01807g
(2019)