Synthesis of potential thrombin inhibitors. Incorporation of tartaric acid templates as P2 proline mimetics
2002 (English)In: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, Vol. 10, no 5, 1567-1580 p.Article in journal (Refereed) Published
With the objective to prepare novel non-peptidic thrombin inhibitors, bioisosteres of the inhibitory tripeptide D-Phe-Pro-Arg chain have been examined. Thus, the P1 Arg was replaced with p-amidinobenzylamine, an elongated homologue of the same and with 2,5-dichloro benzylamine. The P2-P3, D-Phe-Pro, was replaced with a novel tartaric acid template coupled to a series of readily available, mainly lipophilic, amines. Some of these compounds exhibit promising thrombin inhibition activity in vitro, IC50~5.9 µM. © 2002 Elsevier Science Ltd. All rights reserved.
Place, publisher, year, edition, pages
2002. Vol. 10, no 5, 1567-1580 p.
Engineering and Technology
IdentifiersURN: urn:nbn:se:liu:diva-47060DOI: 10.1016/S0968-0896(01)00426-6OAI: oai:DiVA.org:liu-47060DiVA: diva2:267956