Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds
| Autor: | Joanne M. Smallheer, Carolyn A. Weigelt, Shaker A. Mousa, Wayne F. Daneker, Francis J. Woerner, Prabhakar K. Jadhav, Ruth R. Wexler, J S Wells |
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| Rok vydání: | 2004 |
| Předmět: |
Integrins
Stereochemistry Clinical Biochemistry Integrin Drug Evaluation Preclinical Pharmaceutical Science Alpha (ethology) Stereoisomerism Biochemistry Chemical synthesis Drug Discovery Humans Beta (finance) Molecular Biology Binding Sites Bicyclic molecule biology Chemistry Organic Chemistry Imidazoles Antagonist Combinatorial chemistry In vitro biology.protein Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 14:383-387 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2003.10.057 |
| Popis: | Analogues of isoxazoline alpha(v)beta(3) antagonist 1 designed to further restrict the four carbon alkyl tether were prepared by incorporating two spirocyclic scaffolds, 1-oxa-2-azaspiro[4,5]dec-2-ene and 1-oxa-2,7-diazaspiro[4,4]non-2-ene. Additional optimization provided potent antagonists of both alpha(v)beta(3) and alpha(5)beta(1) which are selective over GPIIb/IIIa. |
| Databáze: | OpenAIRE |
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