SAR of N-phenyl piperidine based oral integrin alpha5beta1 antagonists.
Recently, a new class of selective integrin alpha5beta1inhibitors consisting of a heterocyclic based scaffold was published. Herein the SAR and pharmacokinetic profiles of N-phenyl piperidine derivatives are 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; D000631:Aminopyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D004285:Dogs; D015195:Drug Design; D039081:Integrin alpha5beta1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008297:Male; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000631:Aminopyridines; D039081:Integrin alpha5beta1; D010880:Piperidines; D010649:Phenylalanine