Open AccessOxidosqualene Cyclase (OSC) Inhibitors for the Treatment of Dyslipidemia
Author(s) -
Henrietta Dehmlow,
Jean Ackermann,
Johannes D. Aebi,
Denise BlumKaelin,
Alexander Chucholowski,
Philippe Coassolo,
P. G. Hartman,
Manfred Kansy,
Hans Peter Märki,
Olivier Morand,
Elisabeth von der Mark,
Narendra Panday,
A. Ruf,
Ralf Thoma,
Tanja SchulzGasch
Publication year - 2005
Publication title -
chimia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.387
H-Index - 55
eISSN - 2673-2424
pISSN - 0009-4293
DOI - 10.2533/000942905777676858
Subject(s) - candida albicans , chemistry , dyslipidemia , enzyme , in vivo , combinatorial chemistry , biochemistry , computational biology , biology , microbiology and biotechnology , genetics , endocrinology , obesity
Novel inhibitors of oxidosqualene cyclase (OSC) for the treatment of dyslipidemia are reported. Starting point for the chemistry program was a set of compounds derived from a fungicide project which, in addition to high affinity for OSC from Candida albicans, also showed high affinity for the human enzyme (hOSC). Here the evaluation process of different scaffolds is outlined for two representative series, the phenyl substituted benzo[d]isothiazoles and the aminocyclohexanes. The most promising compounds derived from the latter series were further profiled in vivo and showed promising properties with respect to modulation of lipid parameters.