Thiazolidine-2-Thione and 2-Imino-1,3-Dithiolane Derivatives: Synthesis and Evaluation of Antimicrobial Activity
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Pharmaceutical Chemistry Journal, Vol. 54, No. 6, September, 2020 (Russian Original Vol. 54, No. 6, June, 2020)
THIAZOLIDINE-2-THIONE AND 2-IMINO-1,3-DITHIOLANE DERIVATIVES: SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY Mojtaba Ghanbari Mehrabani,1,2,3,5 Kazem Dindar Safa,1,* Mahdi Rahimi,1,3 Maryam Alyari,1 Khudaverdi Ganbarov,4 and Hossein Samadi Kafil5,** Original article submitted November 4, 2019. The emergence of antibiotic resistance is one of the most important public health concerns in the world. To solve this major problem, a series of antimicrobial compounds have been synthesized and tested against bacteria, yeast and fungi microorganisms. Thiazolidines and dithiolanes possess many biological activities against microbial strains. In this study, a facile free-solvent method for the synthesis of thiazolidine derivatives by one-pot reaction was developed and their biological activity was evaluated in comparison to 2-imino-1,3dithiolanes. Microbial inhibition growth effects of the synthesized against microbial species compounds were characterized in terms of disk diffusion and minimum inhibitory concentration (MIC) methods, The MICs of the synthesized compounds were determined and the results showed that almost all synthesized compounds have antimicrobial potential. All thiazolidines are effective candidates for antimicrobial activity against C. albicans and A. niger species and all dithiolanes are strong antibiotics against P. aeruginosa. Keywords: one-pot synthesis, heterocycle, antibacterial activity, antibiotic resistance.
synthetic chemistry, green chemistry, and pharmaceutical chemistry applications for generation of structural diversity and libraries of drug-like molecules. Therefore, the development of new OPRs and improvement of known OPRs for the synthesis of new compounds is an active area of research in synthetic organic chemistry. Thiazolidine-2-thione has conventionally been synthesized in alkaline solution by heating of b-amino alcohol and carbon disulfide. Long reaction times, high temperature, using strong base, and the excess amount of carbon disulfide are disadvantage of this simple procedure. Other synthesis methods previous reported in literature [12, 24, 26, 36] also had some drawbacks Therefore, methods which improve the above-mentioned synthesis are still in demand. Several approaches have been extensively developed for the synthesis and biological activity evaluation of thiazolidine-2-thiones [3, 5, 17, 19, 37]. Various derivatives of thiazolidine are suitable as agents for plant protection [9], protein conjugation [31, 32], reactive groups for drug carriers in drug delivery systems [22], and synthesis of biologically active compounds [14]. In the 1980s, some studies were reported in which 2-imino-1,3-dithiolanes behaved as herbicidal antidotes [18, 33]. However, biological properties of 2-imino-1,3-dithiolane derivatives have not been studied widely and compared with analogs and other heterocyclic
1. INTRODUCTION Thiazolidine-2-thiones and 2-imino-1,3-dithiolanes are represe
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