EFFECTS OF QUINAZOLINE(3H,1H)-4-ONE-2-THIONES WITH AXIAL AND CENTRAL CHIRALITY ON THE CONTRACTILE RESPONSE OF SMOOTH-MUSCLE

Quinazolines are versatile nitrogen heterocyclic compounds displaying a broad spectrum of biological and pharmacological activities. The inf luence of some new synthesized quinazolines with axial and central chi rality was studied on the isometric muscle tension of rat ileum, rat u terus, and porcine coronary artery. While structural changes of the co mpounds showed only little influence on peristaltic movement of the il eum, quinazoline derivatives induced a relaxation in the uterus and in the coronary artery depending on the kind and position of the substit uent. The introduction of axial chirality into the molecule of modific ation of the side chain caused an increase in the pharmacological acti on. These effects could not be inhibited by sympatholytics. So far the mechanisms and receptors causing the spasmolysis are unknown.