Discovery of orally available integrin alpha5beta1 antagonists.

Zischinsky, Gunther; Osterkamp, Frank; Vossmeyer, Doerte; Zahn, Grit; Scharn, Dirk; Zwintscher, Ariane; Stragies, Roland

Zischinsky, Gunther; Osterkamp, Frank; Vossmeyer, Doerte; Zahn, Grit; Scharn, Dirk; Zwintscher, Ariane; Stragies, Roland.

Affiliation

Zischinsky G; Jerini AG, Invalidenstrasse 130, Berlin D-10115, Germany.

Bioorg Med Chem Lett ; 20(1): 380-2, 2010 Jan 01.

Article in En | MEDLINE | ID: mdl-19910191

ABSTRACT

ABSTRACT

Previous research within our laboratories identified the 3-hydroxypyrrolidine scaffold 1 as a new and selective integrin alpha5beta1 inhibitor class which was designed for local administration. Herein the discovery of new orally available integrin alpha5beta1 inhibitor scaffolds for potential systemic treatment is described.

Subject(s)

Integrin alpha5beta1/antagonists & inhibitors; Pyrrolidines/chemistry; Administration, Oral; Animals; Drug Design; Half-Life; Integrin alpha5beta1/metabolism; Male; Pyrrolidines/chemical synthesis; Pyrrolidines/pharmacokinetics; Rats; Rats, Wistar; Structure-Activity Relationship

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Full text: 1 Database: MEDLINE Main subject: Pyrrolidines / Integrin alpha5beta1 Limits: Animals Language: En Year: 2010 Type: Article

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Full text: 1 Database: MEDLINE Main subject: Pyrrolidines / Integrin alpha5beta1 Limits: Animals Language: En Year: 2010 Type: Article