Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.
3-Amino-3-phenylpropionamide derivatives were produced as small molecule mimics of the cyclic octapeptide octreotide from readily available imine 1. The compounds exhibit high affinity for the mu opioid receptor.
Allen
M P
MP
CNS Discovery, Central Research Division, Pfizer Inc, Groton, CT 06340, USA.
Blake
J F
JF
Bryce
D K
DK
Haggan
M E
ME
Liras
S
S
McLean
S
S
Segelstein
B E
BE
D000818:Animals; D001596:Benzylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D001923:Brain Chemistry; D016466:CHO Cells; D006224:Cricetinae; D018360:Crystallography, X-Ray; D015195:Drug Design; D006801:Humans; D008024:Ligands; D015282:Octreotide / Q000031:analogs & derivatives / Q000494:pharmacology; D051381:Rats; D017450:Receptors, Opioid, mu / Q000187:drug effects*
D001596:Benzylamines; D008024:Ligands; D017450:Receptors, Opioid, mu; C045210:3-Tyr-octreotide; D015282:Octreotide