Issue 13, 2014

Synthesis and biological evaluation of XB-1 analogues as novel histamine H3 receptor antagonists and neuroprotective agents

Abstract

A novel class of H3 receptor antagonists, XB-1 analogues based on benzophenone or oxydibenzene scaffolds were synthesized, and their biological activities were evaluated to determine their in vitro neuroprotective effects against Aβ25–35-induced damage in primary cortical neurons and against glutamate-induced neuronal injury in primary cerebellar granule neurons. The results indicated that all of the tested analogues displayed neuroprotective activity at 0.1 μM or 1 μM. These findings may provide new insights into the development of novel promising H3 receptor antagonists with potential neuroprotective activity.

Graphical abstract: Synthesis and biological evaluation of XB-1 analogues as novel histamine H3 receptor antagonists and neuroprotective agents

Supplementary files

Article information

Article type
Paper
Submitted
04 Nov 2013
Accepted
19 Dec 2013
First published
03 Jan 2014

RSC Adv., 2014,4, 6761-6775

Synthesis and biological evaluation of XB-1 analogues as novel histamine H3 receptor antagonists and neuroprotective agents

X. Bao, Y. Jin, X. Liu, H. Liao, L. Zhang and T. Pang, RSC Adv., 2014, 4, 6761 DOI: 10.1039/C3RA46392C

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