Synthesis and Hypolipidemic Activity of Some New Dibenz [c,e] azepine Deravatives

ABSTRACT

Some new 6-substituted 5H-dibenz[c,e]azepine-5,7[6H]-diones [VII] were synthesized and tested for possible hypolipidemic activity. Thus anthranilic acid [I] was converted to diphenic acid [II] which was cyclodehydrated to give diphenic anhydride [III]. Ammonolysis of [III] afforded diphenamic acid [IV] which was cyclodehydrated to yield diphenimide [V]. Potassium salt of [V] was condensed with chloroacetic acid, ethyl chloroacetate or N-substituted and unsubstituted chloroacetamides to produce the target compounds [VII]. The preliminary evaluation of the hypolipidemic activity of [VII] against Triton WR 1339-induced hyperlipidemia in rats showed that several derivatives have demonstrated significant lowering of serum total cholesterol and triglyceride levels at dose of 150 mg/kg comparing with clofibrate