Literature DB >> 22017497

Novel reversible monoamine oxidase A inhibitors: highly potent and selective 3-(1H-pyrrol-3-yl)-2-oxazolidinones.

Sergio Valente1, Stefano Tomassi, Giampiero Tempera, Stefania Saccoccio, Enzo Agostinelli, Antonello Mai.   

Abstract

Monoamine oxidases (MAOs) are involved in various psychiatric and neurodegenerative disorders; hence, MAO inhibitors are useful agents in the therapy of Parkinson's disease, Alzheimer's dementia, and depression syndrome. Herein we report a novel series of 3-(1H-pyrrol-3-yl)-2-oxazolidinones 3-7 as reversible, highly potent and selective anti-MAO-A agents. In particular, 4b, 5b, and 4c showed a K(i-MAO-A) of 0.6, 0.8, and 1 nM, respectively, 4c being 200000-fold selective for MAO-A with respect to MAO-B.

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Year:  2011        PMID: 22017497     DOI: 10.1021/jm201011x

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.

Authors:  Yi-Chao Zheng; Ying-Chao Duan; Jin-Lian Ma; Rui-Min Xu; Xiaolin Zi; Wen-Lei Lv; Meng-Meng Wang; Xian-Wei Ye; Shun Zhu; David Mobley; Yan-Yan Zhu; Jun-Wei Wang; Jin-Feng Li; Zhi-Ru Wang; Wen Zhao; Hong-Min Liu
Journal:  J Med Chem       Date:  2013-11-01       Impact factor: 7.446

2.  A Rh(II)-catalyzed multicomponent reaction by trapping an α-amino enol intermediate in a traditional two-component reaction pathway.

Authors:  Shunying Liu; Wenfeng Yao; Yuan Liu; Qinghua Wei; Jianghui Chen; Xiang Wu; Fei Xia; Wenhao Hu
Journal:  Sci Adv       Date:  2017-03-08       Impact factor: 14.136

3.  One-pot sequential multicomponent reaction between in situ generated aldimines and succinaldehyde: facile synthesis of substituted pyrrole-3-carbaldehydes and applications towards medicinally important fused heterocycles.

Authors:  Anoop Singh; Nisar A Mir; Sachin Choudhary; Deepika Singh; Preetika Sharma; Rajni Kant; Indresh Kumar
Journal:  RSC Adv       Date:  2018-04-24       Impact factor: 4.036

  3 in total

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