title: Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents.
abstract: 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.
authors.affiliation: Pfizer Inc., Groton, CT 06340, USA. jin.li@pfizer.com
authors.forename: Jin
authors.initials: J
authors.lastname: Li
authors.forename: Peter
authors.initials: P
authors.lastname: Bertinato
authors.forename: Hengmiao
authors.initials: H
authors.lastname: Cheng
authors.forename: Bridget M
authors.initials: BM
authors.lastname: Cole
authors.forename: Brian S
authors.initials: BS
authors.lastname: Bronk
authors.forename: Burton H
authors.initials: BH
authors.lastname: Jaynes
authors.forename: Anne
authors.initials: A
authors.lastname: Hickman
authors.forename: Michelle L
authors.initials: ML
authors.lastname: Haven
authors.forename: Nicole L
authors.initials: NL
authors.lastname: Kolosko
authors.forename: Chris J
authors.initials: CJ
authors.lastname: Barry
authors.forename: Tara B
authors.initials: TB
authors.lastname: Manion
mesh_terms: 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
chemical_list: D019440:Anti-Obesity Agents; D002352:Carrier Proteins; C106092:microsomal triglyceride transfer protein