Design and Synthesis of Non-peptide RGD Mimics for Evaluation of Their Utility as Anti-platelet Agents

Design and Synthesis of Non-peptide RGD Mimics for Evaluation of Their Utility as Anti-platelet Agents

Arg-Gly-Asp (RGD) mimics were synthesized and their anti-platelet activity was evaluated. A concise method was developed for the synthesis of the target compounds from dehydroepiandrosterone and Wieland-Miescher and Hajos-Parrish ketones, which are suitable for readily available platform. Among the...

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Bibliographic Details
Published in:Chemical and Pharmaceutical Bulletin Vol. 64; no. 12; pp. 1726 - 1738
Main Authors: Kazuhiro Higuchi, Hideki Hikita, Asumi Murayama, Daichi Yuri, Natsu Kobayakawa, Takashi Takahashi, Shigeru Kojima, Hiroko Ueno, Tomomi Hatakeyama, Airi Kato, Masanori Tayu, Etsuko Oyama, Shigeo Sugiyama, Kazuyuki Ishii, Hidenobu Takahashi, Tomomi Kawasaki
Format: Journal Article
Language:Japanese
Published: Pharmaceutical Society of Japan 01-12-2016
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Summary:Arg-Gly-Asp (RGD) mimics were synthesized and their anti-platelet activity was evaluated. A concise method was developed for the synthesis of the target compounds from dehydroepiandrosterone and Wieland-Miescher and Hajos-Parrish ketones, which are suitable for readily available platform. Among the synthesized compounds, the perhydronaphthalene framework with a 3-(4-piperidinyl)propoxyl structure 3e possessed the highest anti-aggregative activity. The IC50 values of 3e were 0.91 mM (ADP initiation) and 0.54 mM (collagen initiation).
ISSN:0009-2363