Synthesis and antibacterial activity of 9-substituted minocycline derivatives.
A number of 9-acylamino and 9-sulfonylamino derivatives of minocycline have been synthesized for structure-activity relationship studies. These compounds showed activity against both tetracycline-susceptible and tetracycline-resistant strains. Many of the 9-sulfonylamino derivatives exhibited improved antibacterial activity against a number of tetracycline- and minocycline-resistant Gram-positive pathogens.
Sum
Phaik-Eng
PE
Department of Chemical and Screening Sciences, Wyeth Research, Chemical Sciences Building 222/3147, 401 N. Middletown Road, Pearl River, NY 10965, USA. sump@wyeth.com
Ross
Adma T
AT
Petersen
Peter J
PJ
Testa
Raymond T
RT
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000472:pathogenicity; D008911:Minocycline / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D008911:Minocycline