Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase) |
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| Authors: | Ghosh Arun K Devasamudram Thippeswamy Hong Lin DeZutter Christopher Xu Xiaoming Weerasena Vajira Koelsch Gerald Bilcer Geoffrey Tang Jordan |
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| Institution: | Department of Chemistry, University of Illinois at Chicago, 845 West Taylor Street, Chicago, IL 60607, USA. arunghos@uic.edu |
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| 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 (beta-secretase). |
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