title: Synthesis and structure-activity relationship of novel glycylcycline derivatives leading to the discovery of GAR-936.
abstract: A number of new glycylcyclines were synthesized for structure-activity relationship study. Many of the derivatives exhibit potent, broad spectrum antibacterial activity against both tetracycline susceptible and resistant organisms. GAR-936 (TBG-MINO) shows better activity than the previously reported DMG-MINO and DMG-DMDOT.
authors.affiliation: Chemical Sciences, Wyeth-Ayerst Research, Pearl River, New York 10965, USA.
authors.forename: P E
authors.initials: PE
authors.lastname: Sum
authors.forename: P
authors.initials: P
authors.lastname: Petersen
mesh_terms: D013293:Enterococcus faecalis / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008911:Minocycline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013754:Tetracyclines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000078304:Tigecycline
chemical_list: D013754:Tetracyclines; D000078304:Tigecycline; D008911:Minocycline