Dual-acting agents that possess free radical scavenging and antithrombotic activities: Design, synthesis, and evaluation of phenolic tetrahydro-β-carboline RGD peptide conjugates

Wei Bi, Lanrong Bi, Jianhui Cai, Sanguang Liu, Shiqi Peng, Nicholas O Fischer, Jeffrey B H Tok, Guohua Wang

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

A new approach to construct a single dual-acting agent is described. Compounds 6a-c are potent free radical scavengers as demonstrated by the EC50 values in PC12 cell survival assay in term of NO, H2O2, and {radical dot}OH scavenging activity. The Ach-induced vaso-relaxation assay further confirms the potent NO scavenging activity of compounds 6a-c. In addition, 6a-c are efficacious in a rat arterial thrombosis, and are active in ADP- or PAF-induced in vitro platelet aggregation assay, suggesting that compounds 6a-c also possess anti-thrombotic activities. Since both free radical and thrombogenesis are important risk factors in myocardial ischemic/reperfusion injuries, these dual-acting agents having both free radical scavenging and antithrombolic activities may potentially be beneficial toward their treatment.

Original languageEnglish (US)
Pages (from-to)4523-4527
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number17
DOIs
StatePublished - Sep 1 2006
Externally publishedYes

Keywords

  • Anti-thrombotic
  • Dual-action
  • Free radical

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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