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HDAC1/MAO-B dual inhibitors against Alzheimer's disease: Design, synthesis and biological evaluation of N-propargylamine-hydroxamic acid/o-aminobenzamide hybrids

Authors :
Chuansheng Yao
Xiaoying Jiang
Rui Zhao
Zhichao Zhong
Jiamin Ge
Junlong Zhu
Xiang-Yang Ye
Yuanyuan Xie
Zhen Liu
Tian Xie
Renren Bai
Source :
Bioorganic chemistry. 122
Publication Year :
2021

Abstract

A series of N-propargylamine-hydroxamic acid/o-aminobenzamide hybrids inhibitors combining the typical pharmacophores of hydroxamic acid/o-aminobenzamide and propargylamine were designed and synthesized as HDAC1/MAO-B dual inhibitors for the treatment of Alzheimer's disease. Most of the hybrids displayed moderate to good MAO-B inhibitory activities. Among them, Hybrid If exhibited the most potent activity against MAO-B and HDAC1 (MAO-B, IC

Details

ISSN :
10902120
Volume :
122
Database :
OpenAIRE
Journal :
Bioorganic chemistry
Accession number :
edsair.doi.dedup.....d38dc1d11042ddb0fecb4f30b4c00a12