6^th Pharmacovigilance Congress

Biography

Biography: Tariel V Ghochikyan

Abstract

A wide range of biological action and prevalence of lactone-containing compounds in the nature become attractive objects for research by both specialists in fine organic synthesis and pharmacologists. There are numerous drugs used in medicine that contain active aglycones derivatives of γ-lactones. The relevance of research in the field of γ-lactones is confirmed by numerous recent publications. In continuation of our research in this field, we have developed a number of methods for the synthesis of new, earlier not described in literature lactone-containing compounds that can be of certain practical interest. Below there is a graphical scheme of our research. Screening of compounds 1,2 revealed that they displayed inhibitory activity in relation to major phosphatases. It is shown that the inhibitory activity of the main part of studied compounds exceeded similar properties of the known inhibitors levamisil and L-phenylalanine by 17-80 times. Compounds 3 are of certain interest. Their studies have shown that representatives of this class have mainly antibacterial properties were used Gram-positive staphylococci (209P, 93) and gram-negative rods (Sh. Flexner 6858, E coli 0-55), all compounds had moderate anti­bacterial activity. Screening has revealed antimutagenic properties in a series of γ-lactones for the first time (compounds 3, 4). The experiments were carried out on Salmonella tiphimurium TA-100. It was established that with these compounds the number of revertants decreased by 55-60% and mutagenicity factor w        as 2.58-2.7. The same compounds exhibited algicidal activity against filamentous green algae Cladophora. The mentioned compounds in 1 mg/ml concentration destroy cells for 51-60% against 14% of the control preparation monuron. Undoubtedly, compounds 3, 4 can be used in solution of some ecological problems.