title: Synthesis and SAR of azalide 3,6-ketal aromatic derivatives as potent Gram-positive and Gram-negative antibacterial agents.
abstract: 3,6-Ketals of 15-membered azalide pseudoaglycones are a novel series of macrolide antibiotics. The aromatic derivatives of the azalide 3,6-ketals demonstrated potent antibacterial activities against both Gram-positive and Gram-negative bacteria.
authors.affiliation: Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA. henry_cheng@groton.pfizer.com
authors.forename: Hengmiao
authors.initials: H
authors.lastname: Cheng
authors.forename: John P
authors.initials: JP
authors.lastname: Dirlam
authors.forename: Carl B
authors.initials: CB
authors.lastname: Ziegler
authors.forename: Kristin M
authors.initials: KM
authors.lastname: Lundy
authors.forename: Shigeru F
authors.initials: SF
authors.lastname: Hayashi
authors.forename: Barbara J
authors.initials: BJ
authors.lastname: Kamicker
authors.forename: Jason K
authors.initials: JK
authors.lastname: Dutra
authors.forename: Kirsten L
authors.initials: KL
authors.lastname: Daniel
authors.forename: Sheryl L
authors.initials: SL
authors.lastname: Santoro
authors.forename: David M
authors.initials: DM
authors.lastname: George
authors.forename: Camilla D
authors.initials: CD
authors.lastname: Bertsche
authors.forename: Subas M
authors.initials: SM
authors.lastname: Sakya
authors.forename: Melani
authors.initials: M
authors.lastname: Suarez-Contreras
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017963:Azithromycin / Q000031:analogs & derivatives*; D005260:Female; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008413:Mastitis / Q000188:drug therapy; D051379:Mice; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D017963:Azithromycin