259199-34-3Relevant academic research and scientific papers
Novel amidrazone derivatives: Design, synthesis and activity evaluation
Zhou, Hua,Wang, Zhi Sen,Liu, Xin Hua,Chen, Fei Hu
, p. 3158 - 3165 (2018/05/05)
A series of new 6-styryl-naphthalene-2-amidrazone derivatives were synthesized and evaluated as potential ASIC1a inhibitors. Among them, compound 5e showed the most activity to inhibit [Ca2+]i. elevation in acid-induced articular chondrocytes. Together with the important role of ASIC1a in the pathogenesis of tissue acidification diseases including rheumatoid arthritis, these results might provide a meaningful hint or inspiration in developing drugs targeting at tissue acidification diseases.
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.
