Synthesis and antibacterial activity of O-substituted nocathiacin I derivatives.
The synthesis and antibacterial activity of a series of new nocathiacin I derivatives (1-12) containing polar water solubilizing groups is described. Most of these compounds exhibited potent antibacterial activity and have improved water solubility. In addition, compounds 5, 7-9 also exhibited potent in vivo activity.
Naidu
B Narasimhulu
BN
The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. narasimhulu.naidu@bms.com
Sorenson
Margaret E
ME
Hudyma
Thomas
T
Zheng
Xiaofan
X
Zhang
Yunhui
Y
Bronson
Joanne J
JJ
Pucci
Michael J
MJ
Clark
Junius M
JM
Ueda
Yasutsugu
Y
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D013293:Enterococcus faecalis / Q000187:drug effects; D036341:Intercellular Signaling Peptides and Proteins; D008826:Microbial Sensitivity Tests; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D012995:Solubility; D013211:Staphylococcus aureus / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects; D013329:Structure-Activity Relationship; D014867:Water / Q000737:chemistry
D000900:Anti-Bacterial Agents; D036341:Intercellular Signaling Peptides and Proteins; D010455:Peptides; C463319:nocathiacin I; D014867:Water