title: Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform.
abstract: Tetrahydroquinoline A is a potent inhibitor of the cholesterol ester transfer protein (CETP), a target for the treatment of low HDL-C and atherosclerosis. Low HDL-C has been identified as a key risk factor for cardiovascular disease in addition to high LDL-C, the target of the statin drugs. Tetrahydroquinoline A inhibits partially purified CETP with an IC(50) of 39nM. The preparation of a series of potent inhibitors of CETP designed around a 1,2,3,4-tetrahydroquinoline platform will be discussed.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Metabolic Disorders Team, 1000 Route 202, P.O. Box 300, Raritan, NJ 08869, USA.
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Rano
authors.forename: Ellen
authors.initials: E
authors.lastname: Sieber-McMaster
authors.forename: Patricia D
authors.initials: PD
authors.lastname: Pelton
authors.forename: Maria
authors.initials: M
authors.lastname: Yang
authors.forename: Keith T
authors.initials: KT
authors.lastname: Demarest
authors.forename: Gee-Hong
authors.initials: GH
authors.lastname: Kuo