Title of article
Structure-based design of cycloamide–urethane-derived novel inhibitors of human brain memapsin 2 (β-secretase)
Author/Authors
Arun K. Ghosh، نويسنده , , Thippeswamy Devasamudram، نويسنده , , Lin Hong، نويسنده , , Christopher DeZutter، نويسنده , , Xiaoming Xu، نويسنده , , Vajira Weerasena، نويسنده , , Gerald Koelsch، نويسنده , , Geoffrey Bilcer، نويسنده , , Jordan Tang، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
15
To page
20
Abstract
A series of novel macrocyclic amide-urethanes was designed and synthesized based upon the X-ray crystal structure of our lead inhibitor (1, OM99-2 with eight residues) bound to memapsin 2. Ring size and substituent effects have been investigated. Cycloamide–urethanes containing 14- to 16-membered rings exhibited low nanomolar inhibitory potencies against human brain memapsin 2 (β-secretase).
Keywords
Alzheimer’s Disease , inhibitor , Memapsin 2 , Secretase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795141
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