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Can I read Structure–activity studies on diphenylpyrazine derivatives: A novel class of prostacyclin receptor agonists on EtoBox?
Structure–activity studies on diphenylpyrazine derivatives: A novel class of prostacyclin receptor agonists by Tetsuo Asaki; Taisuke Hamamoto; Yukiteru Sugiyama; Keiichi Kuwano; Kenji Kuwabara is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Structure–activity studies on diphenylpyrazine derivatives: A novel class of prostacyclin receptor agonists about?
To develop nonprostanoid prostacyclin receptor agonists with a high degree of metabolic resistance and an extended duration of action, a novel series of diphenylpyrazine derivatives was synthesized and evaluated for their inhibition of ADP-induced human platelet aggregation. Structure-activity relationship studies on the side chain containing the carboxylic acid moiety of the lead compound 5c showed that the length of the linker and the presence of the concatenating nitrogen atom adjacent to the pyrazine ring are critical for the antiaggregatory activity. This study led to the discovery of 2-amino-5,6-diphenylpyrazine derivatives 8c, 15a, and 15b, which showed potent inhibition of platelet aggregation with IC(50) values of 0.2 microM. Among these compounds, 15b is an orally available and long-lasting prostacyclin receptor agonist which is promising for the treatment of various vascular diseases.
Who reads Structure–activity studies on diphenylpyrazine derivatives: A novel class of prostacyclin receptor agonists?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Tetsuo Asaki; Taisuke Hamamoto; Yukiteru Sugiyama; Keiichi Kuwano; Kenji Kuwabara
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2007
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)