title: Synthesis and antibacterial activity of 3-O-carbamoyl derivatives of 6,11-di-O-methylerythromycin A: a novel class of acylides.
abstract: A novel series of acylides, 3-O-carbamoyl derivatives of 6,11-di-O-methylerythromycin A, were synthesized and evaluated for their antibacterial activity. These compounds have significant antibacterial activity against gram-positive pathogens, including erythromycin-resistant but methicillin-susceptible Staphylococcus aureus, erythromycin-resistant and methicillin-resistant S. aureus, erythromycin-resistant Streptococcus pneumoniae, and gram-negative pathogens, such as Haemophilus influenzae. Among the derivatives tested, compounds 4p, 4r, 4w, 4x and 4z were found to have potent activity against most susceptible and resistant bacteria. Compound 4p exhibited excellent antibacterial activity in comparison to the others.
authors.affiliation: State Key Laboratory of Virology, College of Pharmacy, Laojiashan, Wuhan University, Wuhan 430072, China.
authors.forename: Zhongyuan
authors.initials: Z
authors.lastname: Wu
authors.forename: Yong
authors.initials: Y
authors.lastname: Lu
authors.forename: Ming
authors.initials: M
authors.lastname: Luo
authors.forename: Xianran
authors.initials: X
authors.lastname: He
authors.forename: Yuling
authors.initials: Y
authors.lastname: Xiao
authors.forename: Jin
authors.initials: J
authors.lastname: Yang
authors.forename: Yuanhu
authors.initials: Y
authors.lastname: Pan
authors.forename: Guofu
authors.initials: G
authors.lastname: Qiu
authors.forename: Hao
authors.initials: H
authors.lastname: Guo
authors.forename: Hao
authors.initials: H
authors.lastname: Hu
authors.forename: Dingshan
authors.initials: D
authors.lastname: Zhou
authors.forename: Xianming
authors.initials: X
authors.lastname: Hu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D017291:Clarithromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D055808:Drug Discovery; D008826:Microbial Sensitivity Tests
chemical_list: C040935:6,11-di-O-methylerythromycin A; D000900:Anti-Bacterial Agents; D017291:Clarithromycin