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Updated: Jun 12, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Anti-neuroinflammatory activity of 1,5-benzodiazepine derivatives
Sang Keun Ha1, Donthabhaktuni Shobha, Eunjung Moon
1Kyung Hee University, Giheung-gu, Yongin, Gyeonggi-do, Republic of Korea.
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.
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