5,6-diphenylpyridazine derivatives as acyl-CoA : cholesterol acyltransferase inhibitors

Alkyl-5,6-diphenylpyridazine derivatives combining several main features of ACAT inhibitors, such as a long alkyl side chain linked to a heterocycle a nd the o-diphenyl system, were synthesized and tested. Moreover, modeling s tudies on representative terms were performed. Some compounds displayed ACA T inhibition in the micromolar range, both on the enzyme isolated from rat liver microsomes and in cell-free homogenate of murine macrophages.