A number of benzylalkylketones and benzylalkylcarbinols have been synthesized as non-hydrolizable substrate analogues of penicillin acylase (EC 3.5.1.11), and their affinity to the enzyme has been studied. The compounds with plane trigonal carbonyl group (ketones) were established to has bind to the enzyme 20-40 times more tightly than their tetrahedral counterparts with a hydroxyl function (carbinols). 4-Oxo-5-phenylpentanoic acid was found to be one of the most potent reversible competitive inhibitors of penicillin acylase with Ki-31 microM.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
penicillin acylase
12
[inhibition penicillin
4
acylase escherichia
4
escherichia coli
4
coli benzylalkylketones
4
benzylalkylketones benzylalkylcarbinols]
4
benzylalkylcarbinols] number
4
number benzylalkylketones
4
benzylalkylketones benzylalkylcarbinols
4
benzylalkylcarbinols synthesized
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!