Discovery of diarylacrylonitriles as a novel series of small molecule sortase A inhibitors.
On the basis of a hit from random screening, a novel class of small-molecule sortase A inhibitors was generated. The primary structure-activity relationship and the minimal structural requirements for potency were established through structural modifications and molecular modeling studies.
Oh
Ki-Bong
KB
Natural Products Research Institute, College of Pharmacy, Seoul National University, 28 Yungun, Jongro, Seoul 110-460, Korea.
Kim
Soo-Hwan
SH
Lee
Jaekwang
J
Cho
Won-Jea
WJ
Lee
Taeho
T
Kim
Sanghee
S
D000181:Acrylonitrile / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry; D019881:Aminoacyltransferases / Q000037:antagonists & inhibitors*; D001426:Bacterial Proteins; D003546:Cysteine Endopeptidases; D007700:Kinetics; D008958:Models, Molecular; D013329:Structure-Activity Relationship
D001426:Bacterial Proteins; D019881:Aminoacyltransferases; C120542:sortase A; D003546:Cysteine Endopeptidases; D000181:Acrylonitrile