a highly efficient protocol has been developed for the synthesis of 2-hydrazolyl-4-thiazolidinone derivatives installing a one pot three component coupling reaction of an aromatic aldehyde, thiosemicarbazide and maleic anhydride using guanidine hydrochloride as highly inexpensive and environmentally friendly catalyst under solvent free condition at 1200c with good to excellent yields, it offers...

Raltegravir was the first HIV-1 integrase inhibitor that gained FDA approval for use in the treatment of HIV-1 infection. Because of the emergence of IN inhibitor-resistant viral strains, there is a need to identify innovative second-generation IN inhibitors. Previously, we identified 2-thioxo-4-thiazolidinone (rhodanine)-containing compounds as IN inhibitors. Herein, we report the design, synt...

Inflammation is a natural process that is connected to various conditions and disorders such as arthritis, psoriasis, cancer, infections, asthma, etc. Based on the fact that cyclooxygenase isoenzymes (COX-1, COX-2) are responsible for the production of prostaglandins that play an important role in inflammation, traditional treatment approaches include administration of non-steroidal anti-inflam...

According to literature data, thiosemicarbazide and thiazolidinone moieties should enhance biological properties of coumarin. Antioxidant, metal-chelating and antifungal activities of all compounds were investigated and compared to the activity of the starting material, 7-hydroxy-4-methylcoumarin, and were proven to possess potent antioxidant and antifungal activity. In general, thiosemicarbazi...

Searching for new types of biological activities among preliminarily identified hit compounds is a key challenge in modern medicinal chemistry. In our study, previously studied 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl]-propionic acid (Les-6614) was screened antimicrobial, antifungal, anti-allergic, and antitumor activities. Moreover, cytotoxicity, molecular docking, SwissAdm...

Utilization of benzoxazinone for synthesis quinazolinone derivatives with 3-heterocycle side chain. treatment of benzoxazinon 1 with cyano acetohydrazide or thionocarbohydrazide gave the quinazolinone derivatives 2 or 12. quinazolinone 2 has been utilized as synthon for new  pyridinone, oxazet, thiazole, thiazolidinone and quinazolinone derivatives. Thiosemicarbazide and thiosemicarbazone deriv...