1997-01-01·Bioorganic & Medicinal Chemistry Letters
Development of the new potent non-peptide gpIIb/IIIa antagonist NSL-95301 by utilizing combinatorial technique
作者: Yoshio Hayashi ; Jun Katada ; Kiyoko Iijima ; Iwao Ojima ; Tohru Asari ; Akira Tachiki ; Isao Uno ; Takeo Harada
The synthetic study of new non-peptide gpIIb/IIIa antagonist, NSL-95301, is presented.The combinatorial technique was engaged in the lead compound discovery process and optimization process to find (+)-NSL-95301.The IC50 value of collagen induced platelet aggregation inhibitory activity is 92 nM.
Development of potent non-peptide GPIIb/IIIa antagonists with tri-substituted β-amino acid derivatives as a new conformational restriction unit
作者: Yano, M. ; Muramatsu, M. ; Katada, J. ; Takiguchi, Y. ; Harada, T. ; Hayashi, Y. ; Uno, I. ; Miyazaki, H. ; Tachiki, A. ; Ojima, I. ; Yasuda, E. ; Sato, Y. ; Iijima, K. ; Asari, T. ; Okazaki, T.
A symposium.The authors have used combinatorial chem. to identify and optimize a three-component (basic unit-spacer-acidic unit) analog of RGD-type title antagonists, leading to compound (R)-I.
Development of the new potent non-peptide GpIIb/IIIa antagonist NSL-95301 by utilizing combinatorial idea