Glycylcyclines. 1. A new generation of potent antibacterial agents through modification of 9-aminotetracyclines.
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.
Sum
P E
PE
American Cyanamid Company, Medical Research Division, Pearl River, New York 10965.
Lee
V J
VJ
Testa
R T
RT
Hlavka
J J
JJ
Ellestad
G A
GA
Bloom
J D
JD
Gluzman
Y
Y
Tally
F P
FP
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
D000900:Anti-Bacterial Agents; D013754:Tetracyclines; D006033:Glycylglycine