1,3,4-thiadiazole: A Privileged Scaffold for Drug Design and Development

Abstract

: 1,3,4-thiadiazole is a five-membered aromatic heterocycle containing two nitrogen atoms and one sulfur atom. As a privileged scaffold, it has its unique chemical properties and biological characteristics. In the design of drugs, they are widely and flexibly applied by medicinal chemists, and many candidates with therapeutic prospects have been developed. In this review, we focus on 1,3,4-thiadiazole derivatives and their various biological activities reported in the past five years (from 2015 to early 2020), such as anticancer, antibacterial, antifungal, anti-tuberculosis, anti-inflammatory, antivirus, anti-leishmania and other functions. It is believed that this review can provide some new ideas for seeking rational design to develop 1,3,4-thiadiazole based medicinal agents with better activity and lower toxicity.

Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity

“…It has been shown to provide excellent biological activities (e.g., anti-inflammatory, anti-DM, antibacterial, and antitumor activities) to molecules . Moreover, its structural unit, −NC–S–, contains sites that can form strong hydrogen bonds with active hydrogen molecules in receptors . Hence, 1,3,4-thiadiazole might be able to bond with a target protein to enhance the affinity of the parent molecule.…”

“…29 Moreover, its structural unit, −N�C−S−, contains sites that can form strong hydrogen bonds with active hydrogen molecules in receptors. 30 Hence, 1,3,4-thiadiazole might be able to bond with a target protein to enhance the affinity of the parent molecule. Our research team has designed and synthesized some 1,3,4-thiadiazoles as PTP1B inhibitors (Figure 1A).…”

Design, synthesis, biological and computational screening of novel pyridine-based thiadiazole derivatives as prospective anti-inflammatory agents

“…This attribute enhances the prospect of these compounds having low toxicity and increased selectivity [ [23] , [24] , [25] , [26] ]. These characteristics attribute for the incorporation of this ring in drugs including carbonic anhydrase inhibitors-acetazolamide, methazolamide; antiprotozoal drug-megazol; antibacterial drugs-cephazolin, cefazedone, sulfamethizole [ [27] , [28] , [29] ] ( Fig. 1 ).…”

Cooperativity of ESPT and Aggregation-Induced Emission Effects—An Experimental and Theoretical Analysis of a 1,3,4-Thiadiazole Derivative

“…A number of 1,3,4-thiadiazole derivatives have been shown to offer promising antimicrobial, antitumor, or neuroprotective properties [ 2 , 3 , 4 , 5 , 6 ], and several have already entered clinical trials or found practical therapeutic applications [ 7 ]. Numerous 1,3,4-thiadiazole-based molecules have also been considered in the process of designing novel lasers [ 8 ], oxidation inhibitors [ 9 ], and chelating agents for complexation of various d-block metal ions [ 10 ].…”