Study of physicochemical properties of a thiodiazol derivates with antimycobacterial acivities

Abstract

Introduction: Tuberculosis remains one of the most devastating infectious diseases affecting people in different social and age groups. The situation becomes even more complicated with the increasing number of drug-resistant tuberculosis cases, where conventional therapy is no longer effective, and better antimycobacterial drugs either do not exist or are too expensive. The purpose of the study: Study of physicochemical properties of an anti-mycobacterial compound from the group ofthiodiazol derivates.Materials and methods: Melting point determining device Kruss KSP1N & KSP1D, drying cabinet, UV-VIS spectrophotometer, solvents and reagents in accordance with the European Pharmacopoeia. Results: In collaboration with the laboratory of the Institute of Organic Synthesis Chemistry of RM, were synthesized 80 compounds substituted derivatives o f 5-aryl-1 ,3,4-oxadiazoles and thiourea, that were tested for anti-mycobacterial activity against M. tuberculosis in the Southern Research Institute, Birmingham, USA. In the series studied, a major activity (MIC 98%) was recorded for the monosubstituted compound of thiourea with allyl fragment. This compound is shown to be a white powder, with yellow tinge or colorless crystals, specific odor and a bitter taste. There have been made physical and physico-chemical analysis to determine the properties of the compound studied: melting point (119.6°C); solubility - the substance is practically insoluble in water and ethanol, slightly soluble in methanol, soluble in chloroform, acetone, DMSO, DMFA, and acetonitrile. It was determined the water content and the loss on drying (Karl Fischer titration reagent and drying oven), which showed water content of the minor (0.0009% and 0.001%, respectively), which also indicates that the substance is not hygroscopic. Conclusions: Determined physicochemical properties of the studied compound will provide the support in the development of analytical methods and standardisation for this product.