A3 adenosine receptors (ARs) have long been viewed as potential therapeutic targets due to their association with a variety of pathophysiological processes. Development of potent and selective A3AR nucleoside ligands has been an area of interest of medicinal chemists since last two decades. Various prime modifications made on N6 and C-2 position of the adenosine moiety has led to the discovery of some of the most efficacious A3AR ligands. This review is an account of the development of 4'-thionucleosides as A3AR agonists and antagonists by various chemical modifications on the thionucleoside template.
Keywords: A3 adenosine receptor, agonist, antagonist, 4’-thionucleoside, structure-activity relationship.