Rhodanines are recognized as privileged heterocycles in medicinal chemistry. The main achievements include the development of drug-like molecules with numerous biological activities as well as approved drugs. The Furan nucleus is considered one of the promising heterocyclic cores in medicinal chemistry that showed numerous ranges of activity. The combination of several heterocycles in a one molecule commonly provides much more interest in the enhanced activity profile of its analogs than their parent separate constituents. Such conjugates are promising objects for modern medicinal chemistry. In this review paper recent advances in the synthesis and biological activities rhodanine-furan conjugates which its application in the different field of drug discovery.

By the reaction of (4-furan-2-yl-thiazol-2-yl)- 3a and (4-thiophen-2-yl-thiazol-2-yl)- 3b acetonitriles with furfural 4 and 5-arylfurfyrals 5a-g 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives 6a-i were obtained. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was found out that (2E)-3-(2-furyl)-2-[4-(2-furyl)-1,3-thiazol-2-yl]acrylonitrile (6a) and 2-(4-thiophen-2-yl-thiazol-2-yl)-acrylonitriles 6h,i possessed low activity and 2-(4-furan-2-yl-thiazol-2-yl)acrylonitrile derivatives 6b-g showed moderate action. Compounds 6b-g were sensitive to cell lines of MDA-MB-468 and T-47D Breast Cancer. In this case cytotoxic effect was observed with a range of GP = -38.24 –1.28%.

A series of novel 1,3,4-thia(oxa)diazole substituted 2-(2,4-dioxothiazolidine-5-ylidene)-acetamides 3a-c, 4 and 5a-k have been synthesized following the acylation reaction of 2-amino-5-aryl-1,3,4-oxadiazoles, 5-amino-1,3,4-thiadiazole-2-thiol and it’s S-alkylated derivatives with 2-(2,4-dioxothiazolidine-5-ylidene)acetyl chloride in dioxane medium. The functionalization of compounds 3b, 3c, 5d and 5e was carried out on their N3 position under N-alkylation conditions with N-aryl-2-chloroacetamides in DMF/ethanol medium yielded the corresponding 2,4-dioxothiazolidine-3,5-diacetic acid diamides 6a-e and 7a-b. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. The antioxidant activity evaluation in vitro of the synthesized compounds was performed by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. As a result, the highly active compound 4, namely 2-(2,4-dioxothiazolidin-5-ylidene)-N-(5-mercapto-[1,3,4]thiadiazol-2-yl)acetamide was found to be the most efficient candidate among all compounds with a radical scavenging ability of 88.9%, which was comparable that for ascorbic acid (92.7%). The experimentally calculated IC50 value of 43.1 μM for compound 4 was lower than for ascorbic acid (50.5 μM).

УДК: 616–093+547.789

As a result of the furfural reaction with diazonium, salts 1a-h the arylfuran-2-carbaldehydes 3a-h were synthesized. In the reaction of Wilgerodt-Kindler, arylfuran-2-carbaldehydes with sulfur and aryl piperazines was prepared 1-aryl-4-[(5-aryl-2-furyl)carbonothioyl]piperazines. The structures of target compounds 5a-l were confirmed by using 1H NMR spectroscopy and elemental analysis. The antimicrobial activity of the synthesized substances was evaluated by the value of the MIC and minimum fungicidal and bactericidal concentration. The findings exhibited that the compounds
possessed moderate antimicrobial potential. In vitro anticancer activity assessment on the full panel