Medicinal Chemistry and Properties of 1,2,4-Thiadiazoles

Title: Medicinal Chemistry and Properties of 1,2,4-Thiadiazoles

Volume: 5 Issue: 4

Author(s): Tim Fat Tam, Regis Leung-Toung, Wanren Li, Michael Spino and Khashayar Karimian

Affiliation:

Keywords: thiadiazole, proton pump, cathepsin b, factor xiiia, transglutaminase, cysteine thiol, inhibitors

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).

Cite this article as:

Tam Fat Tim, Leung-Toung Regis, Li Wanren, Spino Michael and Karimian Khashayar, Medicinal Chemistry and Properties of 1,2,4-Thiadiazoles, Mini-Reviews in Medicinal Chemistry 2005; 5 (4) . https://dx.doi.org/10.2174/1389557053544056