Synthesis and SAR of azalide 3,6-ketal aromatic derivatives as potent Gram-positive and Gram-negative antibacterial agents.
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.
Cheng
Hengmiao
H
Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA. henry_cheng@groton.pfizer.com
Dirlam
John P
JP
Ziegler
Carl B
CB
Lundy
Kristin M
KM
Hayashi
Shigeru F
SF
Kamicker
Barbara J
BJ
Dutra
Jason K
JK
Daniel
Kirsten L
KL
Santoro
Sheryl L
SL
George
David M
DM
Bertsche
Camilla D
CD
Sakya
Subas M
SM
Suarez-Contreras
Melani
M
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
D000900:Anti-Bacterial Agents; D017963:Azithromycin