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
Letters in Drug Design & Discovery
Title:Synthesis of 3,4–Dihydropyrimidin–2-ones (DHPMs) Using Highly Efficient Recyclable Silica Supported Rhodium Chloride as Heterogeneous Catalyst and their Anti-Neuroinflammatory Activity
Volume: 9 Issue: 10
Author(s): Shobha Donthabhakthuni, Adharvana Chari Murugulla, Prabhakara Chari Murugulla and Kim SunYeou
Affiliation:
Keywords: Aldehydes, Anti-neuroinflammatory, Ethylacetoacetate, Silica supported RhCl3, Urea, 3, 4–dihydropyrimidin– 2-ones, neurodegenerative diseases, Dihydropyrimidinone derivatives, DHPMs, anti-inflammatory actions
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.
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Donthabhakthuni Shobha, Chari Murugulla Adharvana, Chari Murugulla Prabhakara and SunYeou Kim, Synthesis of 3,4–Dihydropyrimidin–2-ones (DHPMs) Using Highly Efficient Recyclable Silica Supported Rhodium Chloride as Heterogeneous Catalyst and their Anti-Neuroinflammatory Activity, Letters in Drug Design & Discovery 2012; 9 (10) . https://dx.doi.org/10.2174/1570180811209050962
DOI https://dx.doi.org/10.2174/1570180811209050962 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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