Synthesis of New N-Mono- and N,N-Dialkylated Imidazole Derivatives and Their Antiplatelet and Anticoagulation Activity

Currently there are several effective synthetic methods for preparing various N -mono- and N , N -dialkylated imidazole derivatives with a very wide variety of biological activities including antiplatelet and anticoagulation effects. The present work reports N -mono- and N , N -dialkylation of 2-methyl-, 2-ethyl-, and 4-nitroimidazoles using (adamantyl-1)bromomethylketone. The synthesized compounds were identified by elemental analyses and PMR and IR spectroscopy. Five compounds having antiplatelet properties were found in in vitro investigations of the antiplatelet and anticoagulation activity in blood of healthy volunteers. The anticoagulation effects of these compounds on the maximum aggregation amplitude were comparable with that of acetylsalicylic acid and even exceeded it with respect to the duration of inhibition of the platelet release reaction.