@article{Saliyeva_Holota_Grozav_Yakovychuk_Lukashchuk_Marushko_Slyvka_Vovk_2021, title={Synthesis, the antiexudative and antimicrobial activity of 6-arylidene substituted imidazo[2,1-b]thiazoles}, volume={19}, url={https://ophcj.nuph.edu.ua/article/view/227378}, DOI={10.24959/ophcj.21.227378}, abstractNote={<p><strong>Aim.</strong> To expand the range of 6-arylidene-2-methyl-2,3-dihydroimidazo[2,1-<em>b</em>]thiazolones as potential objects for studying the antiexudative and antimicrobial activities.</p> <p><strong>Results and discussion.</strong> It has been shown that the condensation of synthetically affordable 2-methyl-2,3-dihydroimidazo[2,1-<em>b</em>]thiazolone with aromatic aldehydes can be successfully used for obtaining the corresponding 6-ylidene-functionalized derivatives. The biological screening of the compounds synthesized revealed that they possessed a low or moderate anti-inflammatory activity and inhibited the inflammation process in the range from 3 to 44 %. During the study of the antimicrobial activity of the substances obtained it was determined that their minimum bacteriostatic and minimum fungistatic concentrations ranged from 31.25 to 250 μg/mL.</p> <p><strong>Experimental part.</strong> The interaction of 2-methyl-2,3-dihydroimidazo[2,1-<em>b</em>]thiazolone with a series of benzaldehydes and salicylic aldehydes in refluxing acetic acid in the presence of anhydrous sodium acetate leads to new 6-arylidene-2-methyl-2,3-dihydroimidazo[2,1-<em>b</em>]thiazolones. The antiexudative activity screening was performed on the model of carrageenan-induced paw oedema of white outbred male rats. The antimicrobial activity of the compounds was studied using the microtechnique of two-fold serial dilutions in a liquid nutrient medium.</p> <p><strong>Conclusions.</strong> It has been found that the Knoevenagel condensation of 2-methyl-2,3-dihydroimidazo[2,1-<em>b</em>]thiazolone with aromatic aldehydes is a convenient way for the structural modification of the position 6 of the heterocyclic system by the arylidene moiety. The arylidene derivatives obtained show a moderate antiexudative activity in the carrageenan-induced rat paw oedema assay, as well as the antimicrobial activity against some gram-positive and gram-negative bacteria and fungi.</p>}, number={2(74)}, journal={Journal of Organic and Pharmaceutical Chemistry}, author={Saliyeva, Lesya M. and Holota, Serhii M. and Grozav, Alina M. and Yakovychuk, Nina D. and Lukashchuk, Mykola M. and Marushko, Larysa P. and Slyvka, Nataliia Yu. and Vovk, Mykhailo V.}, year={2021}, month={Jun.}, pages={29–35} }