Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis of 3,4–Dihydropyrimidin–2-ones (DHPMs) Using Highly Efficient Recyclable Silica Supported Rhodium Chloride as Heterogeneous Catalyst and their Anti-Neuroinflammatory Activity

Author(s): Shobha Donthabhakthuni, Adharvana Chari Murugulla, Prabhakara Chari Murugulla, Kim SunYeou.

Abstract:

The series of 3,4–dihydropyrimidin–2-ones (DHPMs) were synthesized using recyclable silica supported RhCl3 as heterogeneous catalyst and evaluated for anti-neuroinfammatory effect in microglia cells. Among the DHPMs tested, compounds 4g, 4j and 4v strongly inhibited LPS-induced nitric oxide (NO) production with IC50 value of 67.32, 46.01 and 41.31 μM in the microglia cells. Also, compounds 4g, 4j and 4v significantly inhibited the enzyme activity of inducible NO synthase (iNOS) without changes of iNOS protein expression and NO scavenging activity. This result suggests that compounds 4g, 4j and 4v showed the anti-neuroinflammatory effect by suppressing iNOS enzyme activity.

Keywords: Aldehydes, Anti-neuroinflammatory, Ethylacetoacetate, Silica supported RhCl3, Urea, 3, 4–dihydropyrimidin– 2-ones, neurodegenerative diseases, Dihydropyrimidinone derivatives, DHPMs, anti-inflammatory actions

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Article Details

VOLUME: 9
ISSUE: 10
Year: 2012
Page: [962 - 966]
Pages: 5
DOI: 10.2174/1570180811209050962
Price: $58