Synthesis and biological activity of N-substituted aminocarbonyl-1,3-dioxolanes as VLA-4 antagonists

Pyrolidine ring in the N-acylphenylalanine class of VLA-4 antagonists has been successfully replaced by a 1,3-dioxolane and resulting derivative ( 18e) found to be potent in the series. A novel set of compounds with a 1,3-dioxolane ring which acts as a proline bioisostere have been successfully desi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-09, Vol.20 (18), p.5514-5520
Hauptverfasser:	Rehman, Abdul, Soni, Ajay, Naik, Keshav, Nair, Sreeji, Palle, Venkata P., Dastidar, Sunanda, Ray, Abhijit, Alam, M.S., Salman, Mohammad, Cliffe, Ian A., Sattigeri, Viswajanani
Format:	Artikel
Sprache:	eng
Schlagworte:	1,3-Dioxolane Antagonists Bioisosters Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Line Dioxolanes - chemical synthesis Dioxolanes - chemistry Dioxolanes - pharmacology Humans Integrin alpha4beta1 - antagonists & inhibitors Integrin alpha4beta1 - metabolism Medical sciences Models, Molecular Pharmacology. Drug treatments Protein Binding - drug effects Structure-Activity Relationship VLA-4 antagonist
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Zusammenfassung:	Pyrolidine ring in the N-acylphenylalanine class of VLA-4 antagonists has been successfully replaced by a 1,3-dioxolane and resulting derivative ( 18e) found to be potent in the series. A novel set of compounds with a 1,3-dioxolane ring which acts as a proline bioisostere have been successfully designed as VLA-4 receptor antagonists. Compounds ( 18e), ( 28j), and ( 35g) were shown to have high receptor affinities.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.07.069