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Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
- Source :
- Bioorganic & Medicinal Chemistry Letters. 16:845-849
- Publication Year :
- 2006
- Publisher :
- Elsevier BV, 2006.
-
Abstract
- We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin alpha(v)beta3 and show selectivity relative to the other integrins, such as alpha(IIb)beta3 and alpha(v)beta6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
- Subjects :
- Integrins
Stereochemistry
Clinical Biochemistry
Integrin
Drug Evaluation, Preclinical
Administration, Oral
Biological Availability
Pharmaceutical Science
Alpha (ethology)
Platelet Glycoprotein GPIIb-IIIa Complex
Biochemistry
Chemical synthesis
Structure-Activity Relationship
chemistry.chemical_compound
Dogs
Antigens, Neoplasm
Drug Discovery
Animals
Structure–activity relationship
Thiazole
Molecular Biology
Integrin alphaVbeta3
Molecular Structure
biology
Chemistry
Organic Chemistry
Haplorhini
Rats
Bioavailability
Butyrates
Thiazoles
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....9341668d602c5606e629cc594893da77