Thiosemicarbazides in heterocyclization

Abstract

This review summarizes the preparation of substituted thiosemicarbazides with their application with synthesis of important linear and heterocyclic compounds. J. Heterocyclic Chem., (2011).

Synthesis, Antimicrobial Activity and Molecular Docking of Novel Thiourea Derivatives Tagged with Thiadiazole, Imidazole and Triazine Moieties as Potential DNA Gyrase and Topoisomerase IV Inhibitors

“…Thiourea derivatives act as precursors for the synthesis of various classes of acyclic and heterocyclic compounds, in addition to their high biological activity [ 8 ]. Moreover, Thiosemicarbazides are not only intermediate compounds for the synthesis of various bioactive heterocycles such as pyrazole thiazole, thiadiazole, triazole, triazepine, oxadiazole, thiadiazine, thiadiazepine and tetrazole [ 9 , 10 , 11 ] but also has been useful for the design of biologically active agents and could assist as linkers between efficient moieties providing lengths sufficient for nice embedding in the vital receptors. These targets exhibited antiviral, antiamebal, antifungal, antimalarial, antiproliferative and antinociceptive activities [ 12 ].…”

The Synthesis of Thiosemicarbazone-Based Aza-Ylides as Inhibitors of Rat Erythrocyte Glucose 6-Phosphate Dehydrogenase Enzyme

“…In the last years, thiosemicarbazone-appended aromatic compounds have been receiving significant attention in the area of medicine and biochemistry because of their promising biological effects and exceptional pharmacological properties such as antimicrobial (Costello et al, 2008), anti-HIV-1 , anticancer (Jimbow et al, 2000;Yusuf et al, 2014). However, the rich chemistry of thiosemicarbazone (1) and importance of the heterocyclic (Hassan et al, 2011;Gazieva et al, 2012) and metal complexes (Şahin et al, 2010;Netalkar at al., 2015) being steadily derived from this, encourage the further development of the green synthetic methods in this field (Bayindir et al, 2019). A number of popular drugs such as thioacetazone, ambazone (Kleemann et al, 2001) and perchlozone (Smolentsev et al, 2009) are included thiosemicarbazone core (Malkina et al 2017) ( Figure 1).…”

Formation of thiadiazole, thiadiazine, thiadiazepine and pyrazole derivatives in the reaction of 2,4-disubstituted thiosemicarbazides with tetracyanoethylene

“…Carbothioamides and their analogues play a significant role among other nitrogen and sulfur containing compounds used in syntheses of different heterocycles as pyrazoles, 1 1,2,4-triazoles, 2 and 1,3,4-thiadiazoles 1 due to their accessibility and ability to act as bifunctional nucleophiles. [3][4][5][6][7][8][9][10] Metal complexes of thiosemicarbazides display biological activities. [11][12][13] Thiosemicarbazides are derivatives of carbothioamides and contain several nucleophilic centers.…”