title: Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors.
abstract: A novel series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein is described. Optimization of the urea moiety, particularly by incorporation of fluorine, is explored to balance in vitro metabolic stability with CETP potency in the whole plasma assay.
authors.affiliation: Discovery Chemistry, Research and Development, Bristol-Myers Squibb, Princeton, NJ 08543-4000, USA. michael.miller@bms.com
authors.forename: Michael M
authors.initials: MM
authors.lastname: Miller
authors.forename: Yalei
authors.initials: Y
authors.lastname: Liu
authors.forename: Ji
authors.initials: J
authors.lastname: Jiang
authors.forename: James A
authors.initials: JA
authors.lastname: Johnson
authors.forename: Muthoni
authors.initials: M
authors.lastname: Kamau
authors.forename: David S
authors.initials: DS
authors.lastname: Nirschl
authors.forename: Yufeng
authors.initials: Y
authors.lastname: Wang
authors.forename: Lalgudi
authors.initials: L
authors.lastname: Harikrishnan
authors.forename: David S
authors.initials: DS
authors.lastname: Taylor
authors.forename: Alice Ye A
authors.initials: AY
authors.lastname: Chen
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Yin
authors.forename: Ramakrishna
authors.initials: R
authors.lastname: Seethala
authors.forename: Tara L
authors.initials: TL
authors.lastname: Peterson
authors.forename: Tatyana
authors.initials: T
authors.lastname: Zvyaga
authors.forename: Jun
authors.initials: J
authors.lastname: Zhang
authors.forename: Christine S
authors.initials: CS
authors.lastname: Huang
authors.forename: Ruth R
authors.initials: RR
authors.lastname: Wexler
authors.forename: Michael A
authors.initials: MA
authors.lastname: Poss
authors.forename: R Michael
authors.initials: RM
authors.lastname: Lawrence
authors.forename: Leonard P
authors.initials: LP
authors.lastname: Adam
authors.forename: Mark E
authors.initials: ME
authors.lastname: Salvati
mesh_terms: D000588:Amines / Q000097:blood / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054879:Halogenation; D006801:Humans; D051379:Mice; D011725:Pyridines / Q000097:blood / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D014508:Urea / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D000588:Amines; D053480:Cholesterol Ester Transfer Proteins; D011725:Pyridines; D014508:Urea