Inhibition of catalase and epoxide hydrolase by the renal cystogen 2-amino-4,5-diphenylthiazole and its metabolites was written by Hjelle, J. Thomas;Guenthner, Thomas M.;Bell, Kevin;Whalen, Robert;Flouret, George;Carone, Frank A.. And the article was included in Toxicology in 1990.Application In Synthesis of 4,5-Diphenylthiazol-2-amine This article mentions the following:
Subchronic feeding of 2-amino-4,5-diphenyl-1,3-thiazole (DPT) to rats results in the development of renal cysts and has been used as a model system to study polycystic kidney disease. Because previous studies revealed changes in renal enzymes following DPT administration, a possible direct effect of DPT and its phenolic metabolites on catalase and a related enzyme, epoxide hydrolase, was examined Experiments with three in vitro systems (suspensions of rabbit renal tubules, rat kidney homogenates, and com. obtained bovine liver catalase) revealed direct inhibition of catalase activity by the diphenolic metabolite 2-amino-4,5-bis(4′-hydroxyphenyl)-1,3-thiazole (di-OH-DPT), the known renal cystogen nordihydroquaiaretic acid (NDGA), 2-amino-4-(4′-hydroxyphenyl)-5-phenyl-1,3-thiazole (4OH-DPT), and the known catalase inhibitor 2-amino-1,2,4-triazole; DPT did not inhibit catalase activity. Following oral administration to rats of the DPT congeners, 4OH-DPT caused the greatest decrease in both renal catalase and cytosolic epoxide hydrolase (cEH) activities and the shortest time to onset of cystic lesions. In vitro, mouse liver cEH activity was substantially inhibited by 4OH-DPT and diOH-DPT, and NDGA, but not by 2-amino-4-phenyl-5-(4′-hydroxyphenyl)-1,3-thiazole (5OH-DPT) or DPT itself. Microsomal epoxide hydrolase (mEH) activity was inhibited by 4OH-DPT, unaffected by DPT or diOH-DPT, and stimulated 2-fold by 5OH-DPT. Finally, mEH activity was substantially higher in samples of normal human kidney than in samples of kidney derived from a patient with autosomal recessive polycystic kidney disease; no differences were observed in cEH activity in these samples. Although the role of altered catalase and epoxide hydrolase activities in cystogenesis is unknown, DPT-induced cyst formation is associated with loss of these enzyme activities in kidney tissue. This is the first report of an in vivo diminution of cytosolic epoxide hydrolase activity by xenobiotics. In the experiment, the researchers used many compounds, for example, 4,5-Diphenylthiazol-2-amine (cas: 6318-74-7Application In Synthesis of 4,5-Diphenylthiazol-2-amine).
4,5-Diphenylthiazol-2-amine (cas: 6318-74-7) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Application In Synthesis of 4,5-Diphenylthiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica