Background: The guanidine group defines chemical and physicochemical properties of many compounds of medical interest and guanidine-containing derivatives constitute a very important class of therapeutic agents suitable for the treatment of a wide spectrum of diseases. Objective: To review the most important pharmacological properties, mechanisms of action and therapeutic uses of simple guanidine derivatives, cyclic analogues of guanidines as well as peptides, peptidomimetics and peptoids incorporating arginine. Methods: The review presents both the recent patent literature and original papers dealing with guanidine derivatives that show interesting biological activity and emphasizes the newest developing drugs. Conclusion: Recent achievements in the synthesis of guanidine-containing molecules with diverse chemical, biochemical and pharmacological properties make them of great importance to the design and development of novel drugs acting at CNS, anti-inflammatory agents, inhibitors of Na+/H+ exchanger, i...

Introduction: Compounds incorporating guanidine moiety have found many practical applications in diverse areas of chemistry, such as nucleophilic organocatalysis, anion recognition and coordination chemistry. Moreover, guanidine functional group is found in natural products, pharmaceuticals and cosmetic ingredients produced by synthetic methods. Thus, knowledge of their biological activities and therapeutic uses is of utmost importance for researchers involved in drug discovery processes. Areas covered: In this review the authors highlight the continued development and therapeutic applications of newly synthesized guanidine-containing compounds including small peptides and peptidomimetics incorporating arginine. The review presents patents and patent applications filed in the years 2008 – 2012 with emphasis placed on new mechanisms of pharmacological action of guanidine derivatives. Expert opinion: While guanidines are often thought of as strong organic bases and compounds hydrophilic in nature, over the last 4 years there has been an enormous increase in discovery of new promising lead structures with guanidine core, suitable for development of potential drugs acting at central nervous system, anti-inflammatory agents, anti-diabetic and chemotherapeutic agents as well as cosmetics.