Quantitative Structure-Activity Relationships of Renin Inhibitors

A review is presented on quantitative structure-activity relationships (QSARs) of renin inhibitors which have potential as antihypertensive and cardiovascular agents. They inhibit the renin, an enzyme that is involved in the rate-limiting first step of the renin angiotensin system (RAS). Most of the renin inhibitors are peptidomimetics but recently some nonpeptidomimetic renin inhibitors with low molecular weight have also been developed. In both types of renin inhibitors, the QSARs have exhibited that their inhibition activity would largely depend upon the molecular weight of the compounds, van der waals radius related parameters of the substituents, and the localized electronic effects, particularly of the side chain of the residues substituted in the peptides.