Literature DB >> 20537534

Anti-neuroinflammatory activity of 1,5-benzodiazepine derivatives.

Sang Keun Ha1, Donthabhaktuni Shobha, Eunjung Moon, Murugulla A Chari, Kagga Mukkanti, Sung-Hoon Kim, Kwang-Hyun Ahn, Sun Yeou Kim.   

Abstract

A series of 2,3-dihydro-1,5-benzodiazepines were synthesized and evaluated for anti-inflammatory effects in microglia cells. Among the 1,5-benzodiazepines tested, compound 3e strongly inhibited LPS-induced nitric oxide (NO) production, with an IC(50) value of 7.0microM in the microglia cells. Also, compound 3e significantly inhibited the enzymatic activity of inducible NO synthase (iNOS) without changes in iNOS protein expression or NO scavenging activity. This result suggests that compound 3e showed anti-neuroinflammatory effects by suppressing iNOS enzyme activity. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20537534     DOI： 10.1016/j.bmcl.2010.04.133

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Benzodiazepines: Their Use either as Essential Medicines or as Toxics Substances.

Authors:  Edilma Sanabria; Ronald Edgardo Cuenca; Miguel Ángel Esteso; Mauricio Maldonado
Journal:  Toxics       Date:  2021-02-01

2.  Design, Synthesis, and Bioactivity Study of Novel Tryptophan Derivatives Containing Azepine and Acylhydrazone Moieties.

Authors:  Jingjing Zhang; Rongxin Yang; Lili Li; Jianhua Liu; Yuxiu Liu; Hongjian Song; Qingmin Wang
Journal:  Molecules       Date:  2022-10-08       Impact factor: 4.927

3.  Distinct non-inflammatory signature of microglia in post-mortem brain tissue of patients with major depressive disorder.

Authors:  Gijsje J L J Snijders; Marjolein A M Sneeboer; Alba Fernández-Andreu; Evan Udine; Marco P Boks; Paul R Ormel; Amber Berdenis van Berlekom; Hans C van Mierlo; Chotima Bӧttcher; Josef Priller; Towfique Raj; Elly M Hol; René S Kahn; Lot D de Witte
Journal:  Mol Psychiatry       Date:  2020-10-07       Impact factor: 13.437
  3 in total

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