Szabo S, Reynolds E S, Unger S H
J Pharmacol Exp Ther. 1982 Oct;223(1):68-76.
Structure-activity relationships were qualitatively and quantitatively examined for 56 chemicals (e.g., derivatives of propionitrile, acrylonitrile and cysteamine) which caused duodenal ulcer and/or adrenocortical necrosis in rats. For the first time the duodenal ulcerogenic property of numerous chemicals has been studied in a rational and predictive manner. Ulcerogenic activity was most intense in the carbonitriles attached to two or three carbon backbones and diminished by shortening, lengthening, branching, unsaturating, halogenating or hydroxylating the carbon chains. Different modes of action are implied. Adrenocorticolytic potency was associated with unsaturation of the carbon chain and substitution of the nitrile by thiol or amine radicals. An action of these chemicals on the central nervous system has been suggested.
对56种能在大鼠中引发十二指肠溃疡和/或肾上腺皮质坏死的化学物质(如丙腈、丙烯腈和半胱胺的衍生物)进行了结构-活性关系的定性和定量研究。众多化学物质的十二指肠溃疡ogenic特性首次以合理且可预测的方式得到研究。溃疡ogenic活性在连接到两个或三个碳骨架的碳腈中最为强烈,并通过缩短、延长、分支、不饱和化、卤化或羟基化碳链而减弱。这暗示了不同的作用模式。肾上腺皮质溶解效力与碳链的不饱和性以及腈基被硫醇或胺基取代有关。已有人提出这些化学物质对中枢神经系统有作用。