Inhibition of Emulsin byD-Gluconhydroximo-1,5-lactone and Related Compounds

Autor:	Dieter Beer, Andrea Vasella
Rok vydání:	1986
Předmět:	chemistry.chemical_classification Chromatography Organic Chemistry Biochemistry Catalysis Citrate buffer Inorganic Chemistry Hydrolysis Enzyme chemistry Drug Discovery Ic50 values Physical and Theoretical Chemistry IC50 Lactone Nuclear chemistry
Zdroj:	Helvetica Chimica Acta. 69:267-270
ISSN:	1522-2675 0018-019X
DOI:	10.1002/hlca.19860690203
Popis:	At pH 4.5 (citrate buffer), D-gluconhydroximo-lactone (2), the N-methylurethane 3 and the N-phenylurethane 4 inhibit competitively the hydrolysis of p-nitrophenyl β-D-glucopyranoside by emulsin. The IC50 values of 2, 3, and 4 were 1.6 × 10−4, 1.0 × 10−4, and 5.8 × 10−6M, respectively. The Ki values of 2 and 4 were 9.8 × 10−5 and 2.3 × 10−6M, respectively, while D-glucono-1,5-lactone (1) showed IC50 = 1.1 × 10−4M and Ki = 3.7 × 10−5M.
Databáze:	OpenAIRE
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