The synthesis and the study of antimicrobial properties of 5-r,r’-aminometylene derivatives of thiazolidine-2,4-dione and 4-thioxothiazolidine-2-one

Authors

  • G. О. Derkach SHHE «Ivano-Frankivsk National Medical University», Ukraine
  • S. М. Golota Lviv National Medical University named after Danylo Halytsky, Ukraine
  • V. V. Zasidko SHHE «Ivano-Frankivsk National Medical University», Ukraine
  • I. І. Soronovych Lviv National Medical University named after Danylo Halytsky, Ukraine
  • R. V. Kutsyk SHHE «Ivano-Frankivsk National Medical University», Ukraine
  • R. B. Lesyk Lviv National Medical University named after Danylo Halytsky, Ukraine

DOI:

https://doi.org/10.24959/ophcj.16.898

Keywords:

4-thiazolidin(thi)one, 5-aminomethylene derivatives, multiresistance, antimicrobial activity

Abstract

The study is devoted to the rational search of modern potential antimicrobial agents among of 4-thiazolidine(thi)ones. 5-R,R’-Enamin(thi)ones of thiazolidinone series have been tested for design and the initial screening of the antibacterial properties. The use of 5-ethoxymetylene derivatives of thiazolidine-2,4-dione and 4-thioxothiazolidin-2-one as effective “building blocks” for the synthesis of small libraries of bioactive compounds has been proposed. Nucleophilic substitution reactions between 5-ethoxymetylene derivatives and amino alcohols, the primary and secondary functionalized aromatic and heteroaromatic amines, heterocyclic amines (piperidine and substituted pyrazolines) have been studied. The pharmacological screening of the antimicrobial activity for the enamin(thi)ones synthesized on clinical isolates of staphylococci with different resistance mechanisms to protected β-lactams and multiresistance strains of E. coli and Ps. Aeruginosa has been performed. Compounds with a distinct antimicrobial effect have been identified. They can also increase the sensitivity of S. aureus and S. haemolyticus clinical strains to oxacillin, and can be used to create new combined antimicrobial chemotherapeutic agents. The “structure – antimicrobial activity” relationships for design and search for new antimicrobial agents have been analysed.

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Published

2016-09-19

How to Cite

(1)
Derkach G. О.; Golota S. М.; Zasidko, V. V.; Soronovych I. І.; Kutsyk, R. V.; Lesyk, R. B. The Synthesis and the Study of Antimicrobial Properties of 5-r,r’-Aminometylene Derivatives of Thiazolidine-2,4-Dione and 4-Thioxothiazolidine-2-One. J. Org. Pharm. Chem. 2016, 14, 32-37.

Issue

Vol. 14 No. 3(55) (2016)

Section

Original Researches

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Copyright (c) 2016 National University of Pharmacy

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