192437-73-3Relevant academic research and scientific papers
IMIDAZOLYL-SUBSTITUTED AZABENZOPHENONE COMPOUNDS
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Page/Page column 39, (2010/11/26)
The compounds of formula (I) in which X, Y, R1 and R2 have the meanings as given in the description are novel effective inhibitors of the inducible nitric oxide synthase.
Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors
Dehmlow, Henrietta,Aebi, Johannes D.,Jolidon, Synèse,Ji, Yu-Hua,Von der Mark, Elisabeth M.,Himber, Jacques,Morand, Olivier H.
, p. 3354 - 3370 (2007/10/03)
New orally active non-terpenoic inhibitors of human 2,3-oxidosqualene cyclase (hOSC) are reported. The starting point for the optimization process was a set of compounds derived from a fungicide project, which in addition to showing high affinity for OSC from Candida albicans showed also high affinity for human OSC. Common structural elements of these inhibitors are an amine residue and an electrophilic carbonyl C atom embedded in a benzophenone system, which are at a distance of about 10.7 ?. Considering that the keto moiety is in a potentially labile position, modifications of the substitution pattern at the benzophenone as well as annelated heteroaryl systems were explored. Our approach combined testing of the compounds first for increased binding affinity and for increased stability in vitro. Most promising compounds were then evaluated for their efficacy in lowering plasma total cholesterol (TC) and plasma low-density lipoprotein cholesterol (LDL-C) in hyperlipidemic hamsters. In this respect, the most promising compounds are the benzophenone derivative 1·fumarate and the benzo[d]-isothiazol 24·fumarate, which lowered TC by 40% and 33%, respectively.
Tertiary amines
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, (2008/06/13)
Tertiary amines of the formula STR1 wherein A1, A2, A3, A4, L, M, p, T, and Q are as defined herein, have antimycotic and cholesterol-lowering activity.
