Tris carbamic acid esters: inhibitors of cholesterol absorption; inhibitors of ACAT and CEH
申请人:AMERICAN HOME PRODUCTS CORPORATION
公开号:EP0635501A1
公开(公告)日:1995-01-25
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Tris carbamic acid esters of the formula:
where Z is
or -Ar¹-(CR=CR)₁₋₃-Ar², -Ar¹-NR⁷-AR² and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.
抑制胆固醇酯水解酶(CEH)和/或酰基辅酶 A:胆固醇酰基转移酶(ACAT)可抑制胆固醇的酯化,因此可抑制胆固醇的吸收,从而降低血清胆固醇水平。式中的三氨基甲酸酯:
其中 Z 为
或-Ar¹-(CR=CR)₁₋₃-Ar²、-Ar¹-NR⁷-AR²,A 为连接基团,可抑制 CEH 和/或 ACAT 酶(体外)并抑制胆固醇的吸收。