Synthetic Transformations and Medicinal Significance of 1,2,3-Thiadiazoles Derivatives: An Update

Abstract

The 1,2,3-thiadiazole moiety occupies a significant and prominent position among privileged heterocyclic templates in the field of medicine, pharmacology and pharmaceutics due to its broad spectrum of biological activities. The 1,2,3-thiadiazole hybrid structures showed myriad biomedical activities such as antifungal, antiviral, insecticidal, antiamoebic, anticancer and plant activators, etc. In the present review, various synthetic transformations and approaches are highlighted to furnish 1,2,3-thiadiazole scaffolds along with different pharmaceutical and pharmacological activities by virtue of the presence of the 1,2,3-thiadiazole framework on the basis of structure–activity relationship (SAR). The discussion in this review article will attract the attention of synthetic and medicinal researchers to explore 1,2,3-thiadiazole structural motifs for future therapeutic agents.

Green Chemistry in Organic Synthesis: Recent Update on Green Catalytic Approaches in Synthesis of 1,2,4-Thiadiazoles

“…The versatile heterocyclic thiadiazole rings with different isomeric forms, such as 1,2,3-, 1,2,4-, 1,2,5-and 1,3,4-, display substantial therapeutic efficacy against a wide variety of diseases. The 1,2,4-thiadazole scaffolds represent a fivemembered nitrogen-sulfur-containing significant class of core heterocyclic structures of great interest, mainly because of the part of the structural unit of biologically active molecules: a useful intermediate in medicinal chemistry and part of the clinical drugs, which are given in Figure 4 [232][233][234][235][236][237][238][239][240][241][242][243].…”

Unfolding the Antibacterial Activity and Acetylcholinesterase Inhibition Potential of Benzofuran-Triazole Hybrids: Synthesis, Antibacterial, Acetylcholinesterase Inhibition, and Molecular Docking Studies

“…This has attracted the attention of medicinal researchers to develop novel AChE inhibitors. The heterocyclic scaffolds such as benzofuran [18,19], pyrazole [20], lamivudine [21], quinoxaline-sulfonamide [22], oxadiazole [23][24][25][26], triazole [27,28], phenyl-piperazine-based carbodithioates [29][30][31], and thiadiazole [32,33] have drawn significant attraction in the area of medicinal chemistry due to their remarkable pharmacological and biological activities [34,35]. In particular, benzofuran has attracted researchers because it is so frequent in natural products [36].…”

“…Recently, heterocyclic scaffolds containing the benzofuran ring have been reported as potent AChE inhibitors, such as benzofuran-based benzylpyridinium 1a, tacrine-derived benzofuran 1b, coumarin-linked benzofuran 1c, and hydroxypyridinone-containing benzofuran 1d [39][40][41][42] (Figure 2). The heterocyclic scaffolds such as benzofuran [18,19], pyrazole [20], lamivudine [21], quinoxaline-sulfonamide [22], oxadiazole [23][24][25][26], triazole [27,28], phenyl-piperazine-based carbodithioates [29][30][31], and thiadiazole [32,33] have drawn significant attraction in the area of medicinal chemistry due to their remarkable pharmacological and biological activities [34,35]. In particular, benzofuran has attracted researchers because it is so frequent in natural products [36].…”

Exploring the Synthetic Chemistry of Phenyl-3-(5-aryl-2-furyl)- 2-propen-1-ones as Urease Inhibitors: Mechanistic Approach through Urease Inhibition, Molecular Docking and Structure–Activity Relationship

“…Generally, natural and synthetic heterocycles are privileged derivatives [ 7 , 8 ], such as furans [ 9 ], quinoxalines [ 10 ], coumarins [ 11 ], benzimidazoles [ 12 ], heterocyclic sulfonamides [ 13 ], theophyllines [ 14 ], imidazoles [ 15 ], pyrazoles [ 16 ], thiadiazoles [ 17 ], etc., which demonstrate wide-spectrum biological activities in the fields of pharmacology, medicinal chemistry, pharmaceutical chemistry, and pharmaceutics. In the same way, various heterocyclic synthetic compounds have been designed to compete with the growing challenges related to ureolytic microorganisms, including thioureas [ 18 ], triazoles [ 19 ], thiadiazoles [ 20 ], benzimidazoles [ 21 ], hydroxamic acid [ 22 ], phosphoramidate, and thiazolacetamide [ 23 ].…”