SYNTHESIS AND BIOLOGICAL ACTIVITY OF THE HEXALIN MOIETY OF COMPACTIN (ML-236B)

Article abstract of DOI:10.1016/S0040-4039(00)85703-2

Alcohols 14 and 21 and the derived half-glutarate esters 15 and 22 have been prepared and evaluated as inhibitors of HMG CoA reductase.Compound 14, the hexalin moiety of the natural fungal metabolite compactin (ML-236B) and compound 21, its isomeric diene, have essentially no inhibitory properties.Compound 15 and 22 show definite activity, although several orders of magnitude lower than that shown by compactin.