Compounds which inhibit beta-secretase activity and methods of use thereof
申请人:Oklahoma Medical Research Foundation
公开号:US20040121947A1
公开(公告)日:2004-06-24
Compounds inhibit memapsin 2 &bgr;-secretase activity and selectively inhibit memapsin 2 &bgr;-secretase activity relative to memapsin 1 &bgr;-secretase activity. The compounds are employed in methods to inhibit memapsin 2 &bgr;-secretase activity, in the treatment of Alzheimer's disease, in the inhibition of hydrolysis of a &bgr;-secretase site of a &bgr;amyloid precursor protein and to decrease &bgr;-amyloid protein in in vitro samples and in mammals. Proteins of memapsin 2 associated with compounds of the invention are crystallized.
COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
申请人:GHOSH Arun K.
公开号:US20100267609A1
公开(公告)日:2010-10-21
Compounds inhibit memapsin 2 β-secretase activity and selectively inhibit memapsin 2 β-secretase activity relative to memapsin 1 β-secretase activity. The compounds are employed in methods to inhibit memapsin 2 β-secretase activity, in the treatment of Alzheimer's disease, in the inhibition of hydrolysis of a β-secretase site of a β-amyloid precursor protein and to decrease β-amyloid protein in in vitro samples and in mammals. Proteins of memapsin 2 associated with compounds of the invention are crystallized.
Asymmetric borane reduction of ketones promoted by menthopyrazole-zncl<sub>2</sub>complex
The enantioselective reduction of ketones was accomplished by borane in the presence of pyrazole derivatives, particularly 2-methoxymethyl-3-phenyl-1-menthopyrazole (8). The catalysis of zinc chloride makes it possible to lower the reaction temperature below 0 °C, and to promote enantioselectivity.