259199-37-6Relevant articles and documents
Preparation and pharmacological evaluation of novel glycoprotein (Gp) IIb/IIIa antagonists. 1. The selection of naphthalene derivatives
Ono, Shin'ichiro,Inoue, Yoshihisa,Yoshida, Tomohiro,Ashimori, Atsuyuki,Kosaka, Keigo,Imada, Teruaki,Fukaya, Chikara,Nakamura, Norifumi
, p. 1685 - 1693 (2007/10/03)
The synthesis and design using molecular modeling techniques for non- peptide, low molecular weight novel fibrinogen receptor (glycoprotein IIb/IIIa: Gp IIb/IIIa) antagonists, is reported. We used a highly potent serine protease inhibitor, Nafamostat, having an amidinonaphthyl unit as the starting compound. The compounds 4-(6-amidino-2- naphthylaminocarbonyl)phenoxyacetic acid (5a) and 4-(6-amidino-2- naphthalenecarboxamido)phenoxyacetic acid (5b) inhibited adenosin-5'- diphospate (ADP)-induced aggregation of human platelet-rich plasma (PRP) with IC50 values of 0,05 and 0.07 μM, respectively, and had lost their ability to inhibit a variety of serine proteases, including thrombin, factor Xa, plasmin and trypsin.