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Combinatorial Library Synthesis and Biological Evaluation of Pyrazolo[4,3-e][1,4]diazepine as a Potential Privileged Structure

✍ Scribed by Ju-Yeon Lee; Yong-Chul Kim

Publisher: John Wiley and Sons
Year: 2009
Tongue: English
Weight: 380 KB
Volume: 4
Category: Article
ISSN: 1860-7179
DOI: 10.1002/cmdc.200800453

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✦ Synopsis

Abstract

A privileged structure: A library of tetrahydro‐1,4‐pyrazolo‐diazepin‐8(2__H__)‐ones was designed and synthesized to probe the privileged nature of the scaffold. The design strategy included mimicking the three‐dimensional conformations of β‐turn peptides. Screening against P2X~7~R, BACE‐1, and MC4R gave several hit compounds for each target. The results suggest that pyrazolodiazepin‐8‐one may represent a potential privileged scaffold.magnified image

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