Lyttle, Matthew H.; Hocker, Michael D.; Hui, Hon C.; Caldwell, Colby G.; Aaron, Decius T.; Engqvist-Goldstein, Asa; Flatgaard, Jeffrey E.; Bauer, Karin E. published an article on January 7 ,1994. The article was titled 《Isoenzyme-specific glutathione-S-transferase inhibitors: design and synthesis》, and you may find the article in Journal of Medicinal Chemistry.Application In Synthesis of H-Phg-OEt.HCl The information in the text is summarized as follows:
Glutathione-S-transferase (GST) isoenzyme-selective inhibitors H-Glu[Cys(R)-X-OH]-OH [I; R = (CH2)5Me, CH2Ph, CH2C6H4R1-4, R1 = Me, Cl, NO2, CMe3, OMe; X = Gly, β-Ala, (R)-phenylglycine] were designed by an empirically guided strategy. In the first phase, literature data were used to select C-terminal modifications which generated maximum variation in the catalytic efficiency (Vmax/Km) for I used as substrates with different rat GSTs. Also, on the basis of literature data, the sulfhydryl group was functionalized with a selection of alkyl and aryl groups to maximize potential isoenzyme specificity. Affinity chromatog. sorbents were prepared from I which showed isoenzyme selectivity for both rat tissue and recombinant human GST isoenzymes. Some I also showed selective inhibition of GST activity in catalysis of the reaction of 1-chloro-2,4-dinitrobenzene with glutathione (GSH). In the second phase, electronic effects were explored through synthesis of an isostructural series of S-benzyl GSH ligands with different substituents on the aromatic ring. GST isoenzyme specificity for these ligands, measured by binding to derivatized sorbents, varied substantially, with hydrophobic substituents favoring the human GST M1a isoenzyme and electroneg. moieties favoring GST P1. In the third phase, information obtained from testing both series of compounds was combined and used to prepare GSH analogs with chem. features responsible for isoenzyme specificity at both the C-terminus and the sulfur. This approach gave I [R = CH2C6H4Me-4, X = β-Ala; R = CH2C6H4Cl-4, X = (R)-phenylglycine], which showed improved potency while still maintaining selectivity in the inhibition of GSTs. A detailed discussion of the logic used in the selection of functional groups for maximum potency and selectivity is included. After reading the article, we found that the author used H-Phg-OEt.HCl(cas: 59410-82-1Application In Synthesis of H-Phg-OEt.HCl)
H-Phg-OEt.HCl(cas: 59410-82-1) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Application In Synthesis of H-Phg-OEt.HCl They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics