Bobkova L. Synthesis, properties and relationship "structure - activity" in a series of pyridine derivatives and its analogues.

The object - the detection of patterns of relationship between structure and activity (including toxicity) of biologically active pyridine derivatives and its analogs; the purpose - the system for the evaluation of biological effects of new and known derivatives of pyridine and its analogues on the basis of established regularities "structure - activity", "structure - toxicity" for descriptors of their structure and the identification of trends of purposeful synthesis of new effective and low-toxic compounds with desired set of properties; the methods - organic synthesis, physico-chemical, biological, Toxicological, statistical, quantum-chemical, QSAR; the results - Synthesized new biologically active pyridine derivatives: mono - and bis-pyridinium compounds with azomethine (oximes, Schiff bases) and carbamoyl fragments. Were found effective cholinesterase reactivators for introduction. A new strategy of transformation of Quaternary pyridinium salts in pyrolo[1.2-a]pyridines was developed. Were synthesized nitrogenous analogues of pyridine - thiazolo-pyridazinones and cyclopenta[d]pyrimidinediones. For pyridine derivatives studied, a common methodology and the scheme of the analysis of the dependence "structure - toxicity - activity" in which high results of predictions can be achieved by appropriate combination of descriptors. Were established on promising directions of modification of the pyridine rings which allow to carry out purposeful search of low-toxic and effective compounds with a given set of properties. Developed a draft Quality Control Methods for substance Galotrank; introduced - in pharmaceutical and training process; area - pharmacy.