Synthesis and structure-activity relationship of novel glycylcycline derivatives leading to the discovery of GAR-936.
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.
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Chemical Sciences, Wyeth-Ayerst Research, Pearl River, New York 10965, USA.
Petersen
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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
D013754:Tetracyclines; D000078304:Tigecycline; D008911:Minocycline