Antibacterial Activity of Organic Bioisosteres: (Thio)Urea, Benzil and (Thio)Hydantoins.

Abstract

Heterocyclic molecules play an important role in human life. They are very useful in pharmaceuticals, chemotherapeutic agents, dyestuffs, photographics, co-polymers and other products. The hydantoin core has proven to be an important pharmacophore that provides a wide range of biological properties to the diverse hydantoin derivatives. In this paper, we have studied hydantoin and thiohydantoin as well as the starting reactants for their synthesis. Their antimicrobial activity were evaluated on gram (+) and gram (-) bacteria using the well diffusion and dilution method. All products showed interesting antimicrobial activities (with MIC values = 1.25; 2.50; 5.00 and 10 mg / mL) against the pathogenic strains studied. Both products derived from hydantoins have shown good antimicrobial powers: bacteriostatic (Pan> 4) or bactericidal (Pan< or = 4). We note that the 5,5-diphenylhydantoine DPH and 5,5-diphenyl-2-thiohydantoin DPTH were more active than the reagents (urea, thiourea and benzil), in particular the DPTH which has a wider inhibitory and conservative action on all bacteria. This product could be used in the fight against microbial infections.