Aridicins, novel glycopeptide antibiotics. III. Preparation, characterization, and biological activities of aglycone derivatives.
The aglycone and two pseudoaglycones of aridicin A were prepared by selective hydrolysis and characterized, chemically and biologically. These new analogs demonstrate improved activities in vitro over the parent antibiotics against methicillin sensitive and resistant staphylococci. The major determinant of activity is the mannose substituent, the presence of which results in less potent compounds. The analogs have potent activity against enterococci.
Sitrin
R D
RD
Chan
G W
GW
Chapin
F
F
Giovenella
A J
AJ
Grappel
S F
SF
Jeffs
P W
PW
Phillips
L
L
Snader
K M
KM
Nisbet
L J
LJ
D000818:Animals; D000900:Anti-Bacterial Agents; D001439:Bacteroides / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D003013:Clostridium / Q000187:drug effects; D003016:Clostridium perfringens / Q000187:drug effects; D005673:Fusobacterium / Q000187:drug effects; D006020:Glycopeptides / Q000032:analysis / Q000494:pharmacology; D006868:Hydrolysis; D008358:Mannose; D008712:Methicillin; D051379:Mice; D008826:Microbial Sensitivity Tests; D010403:Penicillin Resistance; D013203:Staphylococcal Infections / Q000517:prevention & control
D000900:Anti-Bacterial Agents; D006020:Glycopeptides; C046074:aridicins; D008358:Mannose; D008712:Methicillin