title: Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors.
abstract: A series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein with aminoheterocycles appended onto the N-terminus of the chemotype were explored as urea mimetics. Potent compounds were discovered and were further optimized to improve metabolic stability and PXR transactivation profile.
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA. Electronic address: yufeng.wang@bms.com.
authors.forename: Yufeng
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Wu
authors.initials: W
authors.lastname: Yang
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Heather J
authors.initials: HJ
authors.lastname: Finlay
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Lalgudi S
authors.initials: LS
authors.lastname: Harikrishnan
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Ji
authors.initials: J
authors.lastname: Jiang
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Muthoni G
authors.initials: MG
authors.lastname: Kamau
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Katy
authors.initials: K
authors.lastname: Van Kirk
authors.affiliation: Synthesis & Analysis Technology Team, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: David S
authors.initials: DS
authors.lastname: Nirschl
authors.affiliation: Department of Biology, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: David S
authors.initials: DS
authors.lastname: Taylor
authors.affiliation: Department of Biology, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Alice Ye A
authors.initials: AY
authors.lastname: Chen
authors.affiliation: Department of Biology, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Yin
authors.affiliation: Department of Biology, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Paul G
authors.initials: PG
authors.lastname: Sleph
authors.affiliation: Department of Biology, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Richard Z
authors.initials: RZ
authors.lastname: Yang
authors.affiliation: Department of Preclinical Candidate Optimization, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Christine S
authors.initials: CS
authors.lastname: Huang
authors.affiliation: Department of Biology, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Leonard P
authors.initials: LP
authors.lastname: Adam
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: R Michael
authors.initials: RM
authors.lastname: Lawrence
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Ruth R
authors.initials: RR
authors.lastname: Wexler
authors.affiliation: Department of Chemistry, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
authors.forename: Mark E
authors.initials: ME
authors.lastname: Salvati
mesh_terms: D032701:Biomimetics; D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors*; D004355:Drug Stability; D005021:Ethylamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014508:Urea / Q000737:chemistry
chemical_list: D001713:Biphenyl Compounds; D053480:Cholesterol Ester Transfer Proteins; D005021:Ethylamines; D006571:Heterocyclic Compounds; D011725:Pyridines; D014508:Urea; C506642:CETP protein, human; C010574:biphenyl
keywords: CETP