ABSTRACT
Before the discovery of the mevinic acids as potent inhibitors of HMG-CoA reductase, the rate limiting enzyme of the cholesterol biosynthetic pathway, there was no rational approach to the design and synthesis of potent and efficacious hypocholesterolemic agents. Since this discovery considerable effort has been devoted to the design and synthesis of totally or partially synthetic inhibitors of this enzyme. Today, inhibition of other steps of the biosynthetic pathway is being investigated for the potential to yield novel cholesterol lowering agents. This review will chronicle the efforts made to identify inhibitors of each step in the cholesterol biosynthetic pathway.
