Quantitative structure-activity relationships of antianginal drugs.

Quantitative structure-activity relationships (QSARs) of various classes of antianginal drugs, e.g. nitrates, beta-adrenergic blocking agents (beta-blockers), and calcium channel blockers (calcium antagonists), have been reviewed. This review gives an overall picture of the mode of action of each class of drugs and points out the specific physicochemical and structural properties that govern their activity. It is observed that in almost all kinds of antianginal drugs the lipophilic factor plays an important role and the next important factor seems to be the steric ones. The electronic factors are found to be occasionally important. In the case of beta-blockers, the most common factor that appeared to govern the activity remained the lipophilicity. In nitrates, too, the activity is observed to primarily depend upon the lipophilicity. In calcium channel blockers, however, the dominant effect is seen to be of steric factors. The steric roles may be essential in drug-receptor interactions, which seem to involve both hydrophobic, and to a lesser extent, electronic interactions.