Abstract
1,2,4-Thiadiazole is a distinctive class of small heterocyclic thiol trapping agents that serve as an interesting pharmacophore in the design of inhibitors targeting the cysteine residues of proteins. X-Ray crystal structures of enzyme-inhibitor complex indicate that the cysteine thiol reacts with the N-S bond of the thiadiazole moiety to form a disulfide bond resulting in the inactivation of the enzymes. This review addresses the medicinal chemistry and various properties of 1,2,4-thiadiazoles in their potential as new electrophilic “warheads” for targeting the cysteine residues of biomolecules (e.g, H+ / K+ ATPase), and cysteine-dependent enzymes (e.g., cathepsin B and transglutaminase).
Keywords: thiadiazole, proton pump, cathepsin b, factor xiiia, transglutaminase, cysteine thiol, inhibitors
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