Can I read Probing the Mid-gorge of Cholinesterases with Spacer-modified Bivalent Quinazolinimines Leads to Highly Potent and Selective Butyrylcholinesterase Inhibitors on EtoBox?

Probing the Mid-gorge of Cholinesterases with Spacer-modified Bivalent Quinazolinimines Leads to Highly Potent and Selective Butyrylcholinesterase Inhibitors by Xinyu Chen; Irina G. Tikhonova; Michael Decker is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Probing the Mid-gorge of Cholinesterases with Spacer-modified Bivalent Quinazolinimines Leads to Highly Potent and Selective Butyrylcholinesterase Inhibitors about?

The spacer structure of homobivalent quinazolinimes acting as potent acetyl-(AChE)-and butyrylcholinesterase (BChE) inhibitors was chemically modified introducing tertiary amine and acyl-amide moieties, and the activities at both ChEs were evaluated. Molecular docking was applied to explain the data and probe the capacity of the mid-gorge site of both ChEs. The novel spacer structures considerably alter the biological profile of bivalent quinazolinimines with regard to both inhibitory activity and selectivity. Mutual interaction of binding to the various sites of the enzymes was further investigated by applying also different spacer lengths and ring sizes of the alicycle of the tricyclic quinazolinimines. In order to achieve selectivity toward BChE and to improve inhibitory activities, the spacer structure was optimized and identified a highly potent and selective BChE inhibitor.

Who reads Probing the Mid-gorge of Cholinesterases with Spacer-modified Bivalent Quinazolinimines Leads to Highly Potent and Selective Butyrylcholinesterase Inhibitors?

Author

Xinyu Chen; Irina G. Tikhonova; Michael Decker

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2011

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)