STRUCTURE-FUNCTION ANALYSIS OF ANTIMALARIAL COMPOUNDS.
Progress rept. no. 4 (Annual) 1 Apr 69-31 Mar 70,
SMITH KLINE AND FRENCH LABS PHILADELPHIA PA
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The multiple parameter regression analysis approach pioneered by Prof. Hansch was applied to determine structure-activity relationships of quinolinaminocarbinols and the phenanthrene aminocarbinols as antimalarial agents. Data for avian antimalarial activity of quinolines have been compared with data obtained in mice for related compounds. Mouse data for phenanthrenes have led to mathematical expressions which have permitted predictions for novel phenanthrenes to be made. A study of phototoxicity data in mice of quinoline aminocarbinols did not uncover any useful differences between antimalarial and phototoxicity structure-function relationships. The utility of a three-dimensional graphing technique to exhibit structure-activity relationships was demonstrated in certain situations. Author