Synthesis and Biological Evaluation of 5‐Nitropyrimidine‐2,4‐dione Analogues as Inhibitors of Nitric Oxide and i NOS Activity
Fifty two compounds based on 5‐nitropyrimidine‐2,4‐dione moiety have been synthesized and evaluated for their inhibitory potency on the production of nitric oxide. Among them, compound 36 inhibited the production of nitric oxide (IC 50 : 8.6 μ m ) on lipopolysaccharide‐induced RAW 264.7 cells and i...
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| Veröffentlicht in: | Chemical biology & drug design 2015-03, Vol.85 (3), p.296-299 |
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| container_title | Chemical biology & drug design |
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| creator | Ma, Liang He, Linhong Lei, Lei Liang, Xiaolin Lei, Kai Zhang, Ronghong Yang, Zhuang Chen, Lijuan |
| description | Fifty two compounds based on 5‐nitropyrimidine‐2,4‐dione moiety have been synthesized and evaluated for their inhibitory potency on the production of nitric oxide. Among them, compound
36
inhibited the production of nitric oxide (IC
50
: 8.6
μ
m
) on lipopolysaccharide‐induced RAW 264.7 cells and inducible nitric oxide synthase activity (IC
50
: 6.2
μ
m
), as well as exerted no potential cytotoxicity (IC
50
> 80.0
μ
m
). Docking study confirmed that compound
36
was an inducible nitric oxide synthase inhibitor with perfect binding to the active site of inducible nitric oxide synthase. At a dose of 10 mg/kg, oral administration of
36
possessed protective properties in carrageenan‐induced paw edema of male ICR mice. |
| doi_str_mv | 10.1111/cbdd.12386 |
| format | Article |
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36
inhibited the production of nitric oxide (IC
50
: 8.6
μ
m
) on lipopolysaccharide‐induced RAW 264.7 cells and inducible nitric oxide synthase activity (IC
50
: 6.2
μ
m
), as well as exerted no potential cytotoxicity (IC
50
> 80.0
μ
m
). Docking study confirmed that compound
36
was an inducible nitric oxide synthase inhibitor with perfect binding to the active site of inducible nitric oxide synthase. At a dose of 10 mg/kg, oral administration of
36
possessed protective properties in carrageenan‐induced paw edema of male ICR mice.</description><identifier>ISSN: 1747-0277</identifier><identifier>EISSN: 1747-0285</identifier><identifier>DOI: 10.1111/cbdd.12386</identifier><language>eng</language><ispartof>Chemical biology & drug design, 2015-03, Vol.85 (3), p.296-299</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c766-29b7171fc2bb7cf40755f46726dcac7cf903b9c356b5b1c4841785e3b4c3a9da3</citedby><cites>FETCH-LOGICAL-c766-29b7171fc2bb7cf40755f46726dcac7cf903b9c356b5b1c4841785e3b4c3a9da3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,781,785,27929,27930</link.rule.ids></links><search><creatorcontrib>Ma, Liang</creatorcontrib><creatorcontrib>He, Linhong</creatorcontrib><creatorcontrib>Lei, Lei</creatorcontrib><creatorcontrib>Liang, Xiaolin</creatorcontrib><creatorcontrib>Lei, Kai</creatorcontrib><creatorcontrib>Zhang, Ronghong</creatorcontrib><creatorcontrib>Yang, Zhuang</creatorcontrib><creatorcontrib>Chen, Lijuan</creatorcontrib><title>Synthesis and Biological Evaluation of 5‐Nitropyrimidine‐2,4‐dione Analogues as Inhibitors of Nitric Oxide and i NOS Activity</title><title>Chemical biology & drug design</title><description>Fifty two compounds based on 5‐nitropyrimidine‐2,4‐dione moiety have been synthesized and evaluated for their inhibitory potency on the production of nitric oxide. Among them, compound
36
inhibited the production of nitric oxide (IC
50
: 8.6
μ
m
) on lipopolysaccharide‐induced RAW 264.7 cells and inducible nitric oxide synthase activity (IC
50
: 6.2
μ
m
), as well as exerted no potential cytotoxicity (IC
50
> 80.0
μ
m
). Docking study confirmed that compound
36
was an inducible nitric oxide synthase inhibitor with perfect binding to the active site of inducible nitric oxide synthase. At a dose of 10 mg/kg, oral administration of
36
possessed protective properties in carrageenan‐induced paw edema of male ICR mice.</description><issn>1747-0277</issn><issn>1747-0285</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><recordid>eNo9UMtOwzAQtBBIlMKFL_AZkWI7dpwcS1WgEmoP7T3yK3RRiKs4rcgNiR_gG_kSnILYw-5qtDOjHYSuKZnQWHdGWzuhLM2zEzSiksuEsFyc_u9SnqOLEF4J4VywfIQ-133TbV2AgFVj8T342r-AUTWeH1S9Vx34BvsKi--PryV0rd_1LbyBhcZFhN3y2G28cXjaqEjduygU8KLZgobOt2EgD0QwePUO1h1tAC9Xazw1HRyg6y_RWaXq4K7-5hhtHuab2VPyvHpczKbPiZFZlrBCSyppZZjW0lScSCEqnkmWWaNMRAqS6sKkItNCU8NzTmUuXKq5SVVhVTpGN7-ypvUhtK4qd_EV1fYlJeWQXjmkVx7TS38AnZ9nHw</recordid><startdate>201503</startdate><enddate>201503</enddate><creator>Ma, Liang</creator><creator>He, Linhong</creator><creator>Lei, Lei</creator><creator>Liang, Xiaolin</creator><creator>Lei, Kai</creator><creator>Zhang, Ronghong</creator><creator>Yang, Zhuang</creator><creator>Chen, Lijuan</creator><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>201503</creationdate><title>Synthesis and Biological Evaluation of 5‐Nitropyrimidine‐2,4‐dione Analogues as Inhibitors of Nitric Oxide and i NOS Activity</title><author>Ma, Liang ; He, Linhong ; Lei, Lei ; Liang, Xiaolin ; Lei, Kai ; Zhang, Ronghong ; Yang, Zhuang ; Chen, Lijuan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c766-29b7171fc2bb7cf40755f46726dcac7cf903b9c356b5b1c4841785e3b4c3a9da3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ma, Liang</creatorcontrib><creatorcontrib>He, Linhong</creatorcontrib><creatorcontrib>Lei, Lei</creatorcontrib><creatorcontrib>Liang, Xiaolin</creatorcontrib><creatorcontrib>Lei, Kai</creatorcontrib><creatorcontrib>Zhang, Ronghong</creatorcontrib><creatorcontrib>Yang, Zhuang</creatorcontrib><creatorcontrib>Chen, Lijuan</creatorcontrib><collection>CrossRef</collection><jtitle>Chemical biology & drug design</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ma, Liang</au><au>He, Linhong</au><au>Lei, Lei</au><au>Liang, Xiaolin</au><au>Lei, Kai</au><au>Zhang, Ronghong</au><au>Yang, Zhuang</au><au>Chen, Lijuan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and Biological Evaluation of 5‐Nitropyrimidine‐2,4‐dione Analogues as Inhibitors of Nitric Oxide and i NOS Activity</atitle><jtitle>Chemical biology & drug design</jtitle><date>2015-03</date><risdate>2015</risdate><volume>85</volume><issue>3</issue><spage>296</spage><epage>299</epage><pages>296-299</pages><issn>1747-0277</issn><eissn>1747-0285</eissn><abstract>Fifty two compounds based on 5‐nitropyrimidine‐2,4‐dione moiety have been synthesized and evaluated for their inhibitory potency on the production of nitric oxide. Among them, compound
36
inhibited the production of nitric oxide (IC
50
: 8.6
μ
m
) on lipopolysaccharide‐induced RAW 264.7 cells and inducible nitric oxide synthase activity (IC
50
: 6.2
μ
m
), as well as exerted no potential cytotoxicity (IC
50
> 80.0
μ
m
). Docking study confirmed that compound
36
was an inducible nitric oxide synthase inhibitor with perfect binding to the active site of inducible nitric oxide synthase. At a dose of 10 mg/kg, oral administration of
36
possessed protective properties in carrageenan‐induced paw edema of male ICR mice.</abstract><doi>10.1111/cbdd.12386</doi><tpages>4</tpages></addata></record> |
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| ispartof | Chemical biology & drug design, 2015-03, Vol.85 (3), p.296-299 |
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| source | Wiley Online Library All Journals |
| title | Synthesis and Biological Evaluation of 5‐Nitropyrimidine‐2,4‐dione Analogues as Inhibitors of Nitric Oxide and i NOS Activity |
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