Synthesis and Anticancer Activity of 2-Cyano-N-(furan-2-ylmethyl)-2-(4-oxo-3-arylthiazolidin-2-ylidene)acetamide Derivatives

Russian Journal of Organic Chemistry - 2-(4-Oxo-3-arylthiazolidin-2-ylidene)acetamide derivatives were prepared by the reaction of 2-cyano-N-furan-2-ylmethyl-3-sulfanyl-3-arylaminoacrylamides with...     

Synthesis and Primary Antitumor Screening of 4-[5-(1H-Indol-3-ylmethylidene)-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]butanamides

Russian Journal of Organic Chemistry - A preparative procedure was developed for the synthesis of 4-[5-(1-R-1H-indol-3-ylmethylidene)-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]butanoic acids which...     

Reaction of Carboxylic Acid Hydrazides with 2,2′-(Carbonothioyldisulfanediyl)diacetic acid in Water as a “Green” Synthesis of N-(4-Oxo-2-sulfanylidene-1,3-thiazolidin-3-yl) Carboxamides

Russian Journal of Organic Chemistry - N-(4-Oxo-2-sulfanylidene-1,3-thiazolidin-3-yl)benzamides were synthesized by reaction of substituted benzohydrazides with...     

Synthesis,Biological Evaluation and Molecular Docking Studies of 5-Indolylmethylen-4-oxo-2-thioxothiazolidine Derivatives

Background: Infectious diseases represent a significant global strain on public health security and impact on socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in the crucial need for the discovery and development of novel entities for the infectious treatment with different modes of action that could target both sensitive and resistant strains. Methods: Compounds were synthesized using the classical organic chemistry methods. Prediction of biological activity spectra was carried out using PASS and PASS-based web applications. Pharmacophore modeling in LigandScout software was used for quantitative modeling of the antibacterial activity. Antimicrobial activity was evaluated using the microdilution method. AutoDock 4.2^® software was used to elucidate probable bacterial and fungal molecular targets of the studied compounds. Results: All compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Three compounds were tested against resistant strains MRSA, P. aeruginosa and E. coli and were found to be more potent than MRSA than reference drugs. All compounds demonstrated a higher degree of antifungal activity than the reference drugs bifonazole (6–17-fold) and ketoconazole (13–52-fold). Three of the most active compounds could be considered for further development of the new, more potent antimicrobial agents. Conclusion: Compounds 5b (Z)-3-(3-hydroxyphenyl)-5-((1-methyl-1H-indol-3-yl)methylene)-2-thioxothiazolidin-4-one and 5g (Z)-3-[5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-benzoic acid as well as 5h (Z)-3-(5-((5-methoxy-1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzoic acid can be considered as lead compounds for further development of more potent and safe antibacterial and antifungal agents.     

Synthesis and Antimicrobial Activity of 2-[5-(R-Benzyl)-4-oxo-1,3-thiazolidin-2-ylidene]-3-oxobutanenitrile and [2-(1-Cyano-2-oxopropylidene)-4-oxo-1,3-thiazolidin-5-ylidene]acetic Acid Derivatives

Russian Journal of Organic Chemistry - The reactions of 2-cyano-3-oxobutanethioamide with ethyl 3-aryl-2-bromopropanoates and dialkyl acetylenedicarboxylates afforded a combinatorial library of new...     

Synthesis of 5-(Het)arylidene-3-[2-(4-hydroxyphenyl)ethyl]-2-thioxothiazolidine-4-one Derivatives and Study of Their Antitumor and Anti-Inflammatory Activity

Russian Journal of General Chemistry - The reaction of aromatic and heteroaromatic aldehydes with 3-[2-(4-hydroxyphenyl)ethyl]-2-thioxothiazolidine-4-one was studied. A series of new...     

Synthesis and Antitumor Activity of New 5-Ylidene Derivatives of 3-(Furan-2-ylmethyl)-2-sulfanylidene-1,3-thiazolidin-4-one

Russian Journal of Organic Chemistry - Reactions of 3-(furan-2-ylmethyl)-2-sulfanyidene-1,3-thiazolidin-4-one with aromatic and heterocyclic aldehydes afforded a series of previously unknown...     

Synthesis and Biological Activity of Pyrazolo[1,5-c][1,3]benzoxazines Containing a Thiazolidin-4-one Fragment

Russian Journal of Organic Chemistry - 5-[4-(2-Aryl-1,10b-dihydropyrazolo[1,5-c][1,3]benzoxazin-5-yl)benzylidene]-1,3-thiazolidin-4-ones were synthesized by reactions of...     

Synthesis and Primary Antitumor Screening of 5-Ylidene Derivatives of 3-(Morpholin-4-yl)-2-sulfanylidene-1,3-thiazolidin-4-one

Russian Journal of Organic Chemistry - A preparative procedure has been developed for the synthesis of 3-(morpholin-4-yl)-2-sulfanylidene-1,3-thiazolidin-4-one (3-morpholinorhodanine). Its reaction...     

5-(1,3-Benzothiazol-2-yl)furan-2-carbaldehyde in the Design of Antitumor Agents

Russian Journal of Organic Chemistry - Reactions of 5-(1,3-benzothiazol-2-yl)furan-2-carbaldehyde with 2-acetylfuran, 2-acetylthiophene, and some compounds containing an active methylene group gave...