Discovery of orally available integrin alpha5beta1 antagonists.
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.
Zischinsky
Gunther
G
Jerini AG, Invalidenstrasse 130, Berlin D-10115, Germany.
Osterkamp
Frank
F
Vossmeyer
Doerte
D
Zahn
Grit
G
Scharn
Dirk
D
Zwintscher
Ariane
A
Stragies
Roland
R
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
D039081:Integrin alpha5beta1; D011759:Pyrrolidines; C032519:pyrrolidine