Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).
Compound 1 was identified by high throughput screening as a novel PAI-1 inhibitor. Optimization of the B and C-segments of 1 resulted in a series of structurally simplified compounds with improved potency. The synthesis and SAR data of these compounds are presented here.
Ye
Bin
B
Discovery Research, Berlex Biosciences, 2600 Hilltop Drive, PO Box 4099, Richmond, CA 94804-0099, USA. bin_ye@berlex.com
Bauer
Shawn
S
Buckman
Brad O
BO
Ghannam
Ameen
A
Griedel
Brian D
BD
Khim
Seock-Kyu
SK
Lee
Wheeseong
W
Sacchi
Karna L
KL
Shaw
Kenneth J
KJ
Liang
Amy
A
Wu
Qingyu
Q
Zhao
Zuchun
Z
D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000379:methods; D000432:Methanol / Q000138:chemical synthesis* / Q000494:pharmacology*; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism*; D051381:Rats
D017395:Plasminogen Activator Inhibitor 1; D000432:Methanol