Medicinal chemistry and properties of 1,2,4-thiadiazoles |
| |
Authors: | Tam Tim Fat Leung-Toung Regis Li Wanren Spino Michael Karimian Khashayar |
| |
Affiliation: | Apotex Research, Inc. Medicinal Chemistry Department, 400 Ormont Drive, Toronto, ON, M9L 1N9, Canada. ttam@apotex.com |
| |
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: | |
本文献已被 PubMed 等数据库收录! |
|