title: WITHDRAWN: Novel azithromycin derivatives with the C-4″ bisamide side chains: synthesis and biological evaluation against gram-positive bacteria.
abstract: Novel azithromycin (AZM) derivatives with the C-4″ bisamide side chains were synthesized and evaluated for their in vitro antibacterial activities. The 4″-O-(benzamido)alkyl carbamates showed excellent activity against the erythromycin-susceptible Streptococcus pneumoniae and exhibited greatly improved activity against erythromycin-resistant S. pneumoniae. Among them, compounds 5g and 6g, which had the same electron-withdrawing group, 3,5-dinitrophenyl, on the termination of their C-4″ bisamide side chains, demonstrated the most potent activity against erythromycin-resistant S. pneumoniae expressing the erm gene, the mef gene and the erm and mef genes, showing 128-fold, 33-fold and 32-fold improved activity in comparison with the parent AZM.The Journal of Antibiotics advance online publication, 15 February 2012; doi:10.1038/ja.2012.3.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, PR China.
authors.forename: Wenping
authors.initials: W
authors.lastname: Cui
authors.forename: Lihong
authors.initials: L
authors.lastname: An
authors.forename: Chenchen
authors.initials: C
authors.lastname: Ma
authors.forename: Siti
authors.initials: S
authors.lastname: Ma
authors.forename: Chao
authors.initials: C
authors.lastname: Cong
authors.forename: Xin
authors.initials: X
authors.lastname: Li
authors.forename: Shutao
authors.initials: S
authors.lastname: Ma