Synthesis and anticonvulsant evaluation of some new 2-substituted-3-arylpyrido[2,3- d]pyrimidinones
[Display omitted] A series of 2-substituted-3-arylpyrido[2,3- d]pyrimidinones was prepared for evaluation as potential anticonvulsants. In murine screening, compounds 4a– c having a 2-oxo-2-(4-pyridyl)ethyl group in the 2-position and a 2-substituted phenyl moiety at the 3-position of the pyridopyri...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2004-11, Vol.12 (21), p.5711-5717 |
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| container_issue | 21 |
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| container_title | Bioorganic & medicinal chemistry |
| container_volume | 12 |
| creator | White, David C. Greenwood, Thomas D. Downey, Aaron L. Bloomquist, Jeffrey R. Wolfe, James F. |
| description | [Display omitted]
A series of 2-substituted-3-arylpyrido[2,3-
d]pyrimidinones was prepared for evaluation as potential anticonvulsants. In murine screening, compounds
4a–
c having a 2-oxo-2-(4-pyridyl)ethyl group in the 2-position and a 2-substituted phenyl moiety at the 3-position of the pyridopyrimidinone system displayed the most potent anti-seizure activity in both the maximal electroshock (MES) and pentylenetetrazol (scPTZ) tests at doses in the 3–10
mg/kg range. Compound
4c showed no agonist activity at the GABA
A receptor and was unable to block presynaptic sodium and calcium channels in vitro. |
| doi_str_mv | 10.1016/j.bmc.2004.07.068 |
| format | Article |
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A series of 2-substituted-3-arylpyrido[2,3-
d]pyrimidinones was prepared for evaluation as potential anticonvulsants. In murine screening, compounds
4a–
c having a 2-oxo-2-(4-pyridyl)ethyl group in the 2-position and a 2-substituted phenyl moiety at the 3-position of the pyridopyrimidinone system displayed the most potent anti-seizure activity in both the maximal electroshock (MES) and pentylenetetrazol (scPTZ) tests at doses in the 3–10
mg/kg range. Compound
4c showed no agonist activity at the GABA
A receptor and was unable to block presynaptic sodium and calcium channels in vitro.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2004.07.068</identifier><identifier>PMID: 15465347</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Animals ; Anticonvulsants - chemical synthesis ; Anticonvulsants - therapeutic use ; Anticonvulsants. Antiepileptics. Antiparkinson agents ; Biological and medical sciences ; Drug Evaluation, Preclinical - methods ; Male ; Medical sciences ; Mice ; Mice, Inbred ICR ; Neuropharmacology ; Pharmacology. Drug treatments ; Pyrimidinones - chemical synthesis ; Pyrimidinones - therapeutic use ; Rats ; Seizures - drug therapy</subject><ispartof>Bioorganic & medicinal chemistry, 2004-11, Vol.12 (21), p.5711-5717</ispartof><rights>2004 Elsevier Ltd</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c379t-dfcb5f79c27f8e261cb4df784feb810d54c012728dd29fe23f88ad6c29716f0e3</citedby><cites>FETCH-LOGICAL-c379t-dfcb5f79c27f8e261cb4df784feb810d54c012728dd29fe23f88ad6c29716f0e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmc.2004.07.068$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16172245$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15465347$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>White, David C.</creatorcontrib><creatorcontrib>Greenwood, Thomas D.</creatorcontrib><creatorcontrib>Downey, Aaron L.</creatorcontrib><creatorcontrib>Bloomquist, Jeffrey R.</creatorcontrib><creatorcontrib>Wolfe, James F.</creatorcontrib><title>Synthesis and anticonvulsant evaluation of some new 2-substituted-3-arylpyrido[2,3- d]pyrimidinones</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>[Display omitted]
A series of 2-substituted-3-arylpyrido[2,3-
d]pyrimidinones was prepared for evaluation as potential anticonvulsants. In murine screening, compounds
4a–
c having a 2-oxo-2-(4-pyridyl)ethyl group in the 2-position and a 2-substituted phenyl moiety at the 3-position of the pyridopyrimidinone system displayed the most potent anti-seizure activity in both the maximal electroshock (MES) and pentylenetetrazol (scPTZ) tests at doses in the 3–10
mg/kg range. Compound
4c showed no agonist activity at the GABA
A receptor and was unable to block presynaptic sodium and calcium channels in vitro.</description><subject>Animals</subject><subject>Anticonvulsants - chemical synthesis</subject><subject>Anticonvulsants - therapeutic use</subject><subject>Anticonvulsants. Antiepileptics. Antiparkinson agents</subject><subject>Biological and medical sciences</subject><subject>Drug Evaluation, Preclinical - methods</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred ICR</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyrimidinones - chemical synthesis</subject><subject>Pyrimidinones - therapeutic use</subject><subject>Rats</subject><subject>Seizures - drug therapy</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1r3DAQQEVpaDZJf0AvxZf2FLmSLEsWPYXQLwjk0PZUipClEdViS1tL3rL_Plp2IbcehpmBN8PMQ-gNJS0lVHzYtuNsW0YIb4lsiRheoA3lguOuU_Ql2hAlBkwGJS7RVc5bQgjjir5Cl7Tnou-43CD7_RDLH8ghNya6GiXYFPfrlGvZwN5MqykhxSb5JqcZmgj_GobzOuYSylrA4Q6b5TDtDktw6Re77XDjfh-7ObgQU4R8gy68mTK8Pudr9PPzpx_3X_HD45dv93cP2HZSFey8HXsvlWXSD8AEtSN3Xg7cwzhQ4npuCWWSDc4x5YF1fhiME5YpSYUn0F2j96e9uyX9XSEXPYdsYZpMhLRmLYTigvS8gvQE2iXlvIDXu3pu_UJToo9m9VZXs_poVhOpq9k68_a8fB1ncM8TZ5UVeHcGTLZm8ouJNuRnTlDJGO8r9_HEQVWxD7DobANECy4sYIt2KfznjCdz-5fc</recordid><startdate>20041101</startdate><enddate>20041101</enddate><creator>White, David C.</creator><creator>Greenwood, Thomas D.</creator><creator>Downey, Aaron L.</creator><creator>Bloomquist, Jeffrey R.</creator><creator>Wolfe, James F.</creator><general>Elsevier Ltd</general><general>Elsevier Science</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20041101</creationdate><title>Synthesis and anticonvulsant evaluation of some new 2-substituted-3-arylpyrido[2,3- d]pyrimidinones</title><author>White, David C. ; Greenwood, Thomas D. ; Downey, Aaron L. ; Bloomquist, Jeffrey R. ; Wolfe, James F.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c379t-dfcb5f79c27f8e261cb4df784feb810d54c012728dd29fe23f88ad6c29716f0e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Animals</topic><topic>Anticonvulsants - chemical synthesis</topic><topic>Anticonvulsants - therapeutic use</topic><topic>Anticonvulsants. Antiepileptics. Antiparkinson agents</topic><topic>Biological and medical sciences</topic><topic>Drug Evaluation, Preclinical - methods</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred ICR</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyrimidinones - chemical synthesis</topic><topic>Pyrimidinones - therapeutic use</topic><topic>Rats</topic><topic>Seizures - drug therapy</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>White, David C.</creatorcontrib><creatorcontrib>Greenwood, Thomas D.</creatorcontrib><creatorcontrib>Downey, Aaron L.</creatorcontrib><creatorcontrib>Bloomquist, Jeffrey R.</creatorcontrib><creatorcontrib>Wolfe, James F.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>White, David C.</au><au>Greenwood, Thomas D.</au><au>Downey, Aaron L.</au><au>Bloomquist, Jeffrey R.</au><au>Wolfe, James F.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and anticonvulsant evaluation of some new 2-substituted-3-arylpyrido[2,3- d]pyrimidinones</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2004-11-01</date><risdate>2004</risdate><volume>12</volume><issue>21</issue><spage>5711</spage><epage>5717</epage><pages>5711-5717</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
A series of 2-substituted-3-arylpyrido[2,3-
d]pyrimidinones was prepared for evaluation as potential anticonvulsants. In murine screening, compounds
4a–
c having a 2-oxo-2-(4-pyridyl)ethyl group in the 2-position and a 2-substituted phenyl moiety at the 3-position of the pyridopyrimidinone system displayed the most potent anti-seizure activity in both the maximal electroshock (MES) and pentylenetetrazol (scPTZ) tests at doses in the 3–10
mg/kg range. Compound
4c showed no agonist activity at the GABA
A receptor and was unable to block presynaptic sodium and calcium channels in vitro.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>15465347</pmid><doi>10.1016/j.bmc.2004.07.068</doi><tpages>7</tpages></addata></record> |
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| subjects | Animals Anticonvulsants - chemical synthesis Anticonvulsants - therapeutic use Anticonvulsants. Antiepileptics. Antiparkinson agents Biological and medical sciences Drug Evaluation, Preclinical - methods Male Medical sciences Mice Mice, Inbred ICR Neuropharmacology Pharmacology. Drug treatments Pyrimidinones - chemical synthesis Pyrimidinones - therapeutic use Rats Seizures - drug therapy |
| title | Synthesis and anticonvulsant evaluation of some new 2-substituted-3-arylpyrido[2,3- d]pyrimidinones |
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