title: Discovery of orally available integrin alpha5beta1 antagonists.
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.
authors.affiliation: Jerini AG, Invalidenstrasse 130, Berlin D-10115, Germany.
authors.forename: Gunther
authors.initials: G
authors.lastname: Zischinsky
authors.forename: Frank
authors.initials: F
authors.lastname: Osterkamp
authors.forename: Doerte
authors.initials: D
authors.lastname: Vossmeyer
authors.forename: Grit
authors.initials: G
authors.lastname: Zahn
authors.forename: Dirk
authors.initials: D
authors.lastname: Scharn
authors.forename: Ariane
authors.initials: A
authors.lastname: Zwintscher
authors.forename: Roland
authors.initials: R
authors.lastname: Stragies
mesh_terms: D000284:Administration, Oral; D000818:Animals; D015195:Drug Design; D006207:Half-Life; D039081:Integrin alpha5beta1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008297:Male; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D039081:Integrin alpha5beta1; D011759:Pyrrolidines; C032519:pyrrolidine