title: Glycylcyclines. 1. A new generation of potent antibacterial agents through modification of 9-aminotetracyclines.
abstract: This report describes the discovery of a new generation of tetracycline antibacterial agents, the "glycylcyclines". These agents are notable for their activity against a broad spectrum of tetracycline-susceptible and -resistant Gram-negative and Gram-positive aerobic and anaerobic bacteria possessing various classes of tetracycline-resistant determinants [tet B (efflux), tet M (ribosomal protection)]. The design and synthesis of a number of 7-substituted 9-substituted-amido 6-demethyl-6-deoxytetracyclines are described.
authors.affiliation: American Cyanamid Company, Medical Research Division, Pearl River, New York 10965.
authors.forename: P E
authors.initials: PE
authors.lastname: Sum
authors.forename: V J
authors.initials: VJ
authors.lastname: Lee
authors.forename: R T
authors.initials: RT
authors.lastname: Testa
authors.forename: J J
authors.initials: JJ
authors.lastname: Hlavka
authors.forename: G A
authors.initials: GA
authors.lastname: Ellestad
authors.forename: J D
authors.initials: JD
authors.lastname: Bloom
authors.forename: Y
authors.initials: Y
authors.lastname: Gluzman
authors.forename: F P
authors.initials: FP
authors.lastname: Tally
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016983:Enterococcus / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D006033:Glycylglycine / Q000737:chemistry* / Q000494:pharmacology; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013753:Tetracycline Resistance; D013754:Tetracyclines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D013754:Tetracyclines; D006033:Glycylglycine