Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents.
We have successfully identified a number of novel MTP inhibitors with single digit nanomolar potency. Analogues 10aq and 10dq demonstrated in vivo efficacy in a murine gut retention assay.
Li
Jin
J
Pfizer Inc., Groton, CT 06340, USA. jin.li@pfizer.com
Bertinato
Peter
P
Cheng
Hengmiao
H
Cole
Bridget M
BM
Bronk
Brian S
BS
Jaynes
Burton H
BH
Hickman
Anne
A
Haven
Michelle L
ML
Kolosko
Nicole L
NL
Barry
Chris J
CJ
Manion
Tara B
TB
D000284:Administration, Oral; D000818:Animals; D019440:Anti-Obesity Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D019440:Anti-Obesity Agents; D002352:Carrier Proteins; C106092:microsomal triglyceride transfer protein