Abstract

Separating the stereospecific factor from others governing the manifestation of biological activity to estimate its relative significance is the first step in understanding the stereospecific effect of biologically active compounds. In certain cases, this can be performed by means of quantitative analysis of structure-activity relationship of congeneric series of bioactive compounds using physical-organic models and multiple regression analysis. Examinations were made for the use of the Hancock Esc values as the model of intra- as well as inter-molecular steric effects. A new procedure to analyze the steric effect in various physical-organic reactivities was proposed. The procedure was successfully extended to analyzing the steric effect between quaternary ammonium cationic head of acetylcholine and its analogs and their target, acetylcholinesterase. Other examples where Esc values are applicable in structure-activity correlations are briefly reviewed. A comparison is made between Esc and other steric parameters currently used in structure-activity studies.

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