Azalide 3,6-Ketals: antibacterial activity and structure–Activity relationships of aryl and hetero aryl substituted analogues

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 7; pp. 1373 - 1375
• Main Authors: Sakya, Subas M, Bertinato, Peter, Pratt, Bryan, Suarez-Contreras, Melani, Lundy, Kristin M, Minich, Martha L, Cheng, Hengmiao, Ziegler, Carl B, Kamicker, Barbara J, Hayashi, Shigeru F, Santoro, Sheryl L, George, David M, Bertsche, Camilla D
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 07.04.2003; Elsevier
• Subjects: Animals; Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - pharmacology; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Biological and medical sciences; Cattle; Cattle Diseases - microbiology; Female; Gonadotropin-Releasing Hormone - analogs & derivatives; Gonadotropin-Releasing Hormone - chemical synthesis; Gonadotropin-Releasing Hormone - pharmacology; Heterocyclic Compounds - chemical synthesis; Heterocyclic Compounds - pharmacology; Mastitis, Bovine - microbiology; Medical sciences; Mice; Microbial Sensitivity Tests; Pasteurella multocida - drug effects; Pasteurellosis, Pneumonic - microbiology; Pharmacology. Drug treatments; Staphylococcus aureus - drug effects; Structure-Activity Relationship; Escherichia coli; Rodentia; Lactone; In vitro; Macrolide; Spiran; Macrocycle; Pasteurella multocida; Pasteurellaceae; Acetal; In vivo; Vertebrata; Mammalia; Structure activity relation; Mouse; Animal; Bacteria; Micrococcales; Micrococcaceae; Antibacterial agent; Chemical synthesis; Staphylococcus aureus; Enterobacteriaceae; Oxygen nitrogen heterocycle
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(03)00100-8

Aryl and hetero aryl substituted 3,6-ketals of 15-membered azalide analogues were synthesized and were found to have potent in vitro antibacterial activity against veterinary pathogens, including Staphylococcus aureus and Pasteurella multocida. Aryl and hetero aryl substituted 3,6-ketals of 15-membered azalide analogues were synthesized and were found to have potent in vitro antibacterial activity against veterinary pathogens, including Staphylococcus aureus and Pasteurella multocida.