Синтез і дослідження антимікробних властивостей 5-R,R’-амінометиленпохідних тіазолідин- 2,4-діону та 4-тіоксотіазолідин-2-ону

• Date: 2016
• Main Authors: Derkach, G. О., Golota, S. М., Zasidko, V. V., Soronovych, I. І., Kutsyk, R. V., Lesyk, R. B.
• Format: Article
• Language: English
• Published: National University of Pharmacy 2016
• Subjects: 4-тіазолідин(ті)они; 5-амінометиленпохідні; мультирезистентність; антимікробна активність; УДК 616-093 547.789
• Online Access: https://ophcj.nuph.edu.ua/article/view/ophcj.16.898
• Journal Title: Journal of Organic and Pharmaceutical Chemistry

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.