title: Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
abstract: This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties.
authors.affiliation: Centro de Investigación Lilly, Alcobendas, Madrid, Spain. escribano@lilly.com
authors.forename: Ana
authors.initials: A
authors.lastname: Escribano
authors.forename: Ana I
authors.initials: AI
authors.lastname: Mateo
authors.forename: Eva M
authors.initials: EM
authors.lastname: Martin de la Nava
authors.forename: Daniel R
authors.initials: DR
authors.lastname: Mayhugh
authors.forename: Sandra L
authors.initials: SL
authors.lastname: Cockerham
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Beyer
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Schmidt
authors.forename: Guoqing
authors.initials: G
authors.lastname: Cao
authors.forename: Youyan
authors.initials: Y
authors.lastname: Zhang
authors.forename: Timothy M
authors.initials: TM
authors.lastname: Jones
authors.forename: Anthony G
authors.initials: AG
authors.lastname: Borel
authors.forename: Stephanie A
authors.initials: SA
authors.lastname: Sweetana
authors.forename: Ellen A
authors.initials: EA
authors.lastname: Cannady
authors.forename: Nathan B
authors.initials: NB
authors.lastname: Mantlo
mesh_terms: D000818:Animals; D016632:Apolipoprotein A-I / Q000235:genetics / Q000378:metabolism; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D008076:Cholesterol, HDL / Q000187:drug effects / Q000378:metabolism; D004285:Dogs; D015195:Drug Design; D005260:Female; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008822:Mice, Transgenic; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D016632:Apolipoprotein A-I; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL; D000960:Hypolipidemic Agents; D011804:Quinolines; D013777:Tetrazoles; C542964:1,2,3,4-tetrahydroquinoline