Journal of Medicinal Chemistry p. 1245 - 1253 (1984)
Update date:2022-08-04
Topics:
Ashton, Michael J.
Ashford, Alan
Loveless, Anthony H.
Riddell, David
Salmon, John
Stevenson, Gregory V.W.
A series of <α-(heterocyclyl)benzyl>piperazines was synthesized and their effect of reducing serum cholesterol and triglyceride levels in the rat was evaluated.A systematic exploration of the structure-activity relationships led to the synthesis of (R,S)-(3,5-dimethylisoxazol-4-yl)<4-(1-methylethyl)phenyl>(4-methylpiperazin-1-yl)methane dihydrochloride (M and B 31426), which had potent activity in lowering serum lipid levels at a daily oral dose of 2 mg/kg and was 100 times more potent than clofibrate.
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