Registration Number
0220U104428,
0120U104045
, R & D reports
Title
The evaluation of biological activity and mechanism of action among novel thiazolidinone derivatives as promissing antimicrobial agents
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Head
Lesyk Roman B., Доктор фармацевтичних наук
Registration Date
17-12-2020
Organization
Danylo Halytsky Lviv National Medical University
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Synthesis of drug-like molecules was performed by conjugation of 4-thiazolidinone or thiazole moieties with known "biophore" heterocyclic systems, in particular the indole and triazole which allows to preserve the pharmacological profile of these compounds and to analyze the structure-activity relationship. Based on the logical-structural approach, the optimal directions of synthesis and structural modification of the target compounds under the conditions of Knovenagel condensation, [2+3]-cyclocondensation reactions, N-alkylation reactions, aminolysis, acylation were established. A focused sub-library of thiazolidine-indole hybrid molecules and a number of new thiazolo[3,2-b][1,2,4]triazol-6-ones have been designed and synthesized. The new compounds were obtained on the basis of multistage syntheses based on 1H-[1,2,4]triazole-3-thiole, 5-ethoxymethylenethiazolo[3,2-b][1,2,4]triazol-6-one, 2-thioxo-thiazolidin-2-one and their 3-substituted derivatives, and using approaches of isosteric replacement and rescafolding. Determining the toxicity parameters of the test compounds allowed to consider them as potential antimicrobial agents for further pharmacological studies. Analysis of the structure-activity relationship allowed to outline the directions of chemical optimization of the identified hit-compounds.
Product Description
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Kryshchyshyn-Dylevych Anna P.
Lozynskyi Andrii V.
Roman Oleksandra M.
Subtelna Ivanna Yu.
Yushyn Ihor M.
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2020-12-17
