Studies on cerebral protective agents. II: Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities
In a search for new cerebral protective agents with anti-anoxic (AA) and anti-lipid peroxidation (ALP) activities, a series of 4-arylpyrimidines, bearing an amino moiety in the C-5 position of the pyrimidine nucleus, was synthesized and tested for AA and ALP activities. Among them, 6-methyl-5-(4-met...
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| Veröffentlicht in: | Chemical & pharmaceutical bulletin 1992, Vol.40 (9), p.2423-2431 |
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| container_end_page | 2431 |
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| container_issue | 9 |
| container_start_page | 2423 |
| container_title | Chemical & pharmaceutical bulletin |
| container_volume | 40 |
| creator | KUNO, A SUGIYAMA, Y KATSUTA, K SAKAI, H TAKASUGI, H |
| description | In a search for new cerebral protective agents with anti-anoxic (AA) and anti-lipid peroxidation (ALP) activities, a series of 4-arylpyrimidines, bearing an amino moiety in the C-5 position of the pyrimidine nucleus, was synthesized and tested for AA and ALP activities. Among them, 6-methyl-5-(4-methylpiperazin-1-ylcarbonyl)-4-(3-nitrophenyl )-2-phenylpyrimidin e (41, FK360) was most effective on both assays and on arachidonate-induced cerebral edema in rats. Structure-activity relationships in regard to AA activity of this series of compounds are also discussed. |
| doi_str_mv | 10.1248/cpb.40.2423 |
| format | Article |
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Among them, 6-methyl-5-(4-methylpiperazin-1-ylcarbonyl)-4-(3-nitrophenyl )-2-phenylpyrimidin e (41, FK360) was most effective on both assays and on arachidonate-induced cerebral edema in rats. 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II: Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities</title><title>Chemical & pharmaceutical bulletin</title><addtitle>Chem Pharm Bull (Tokyo)</addtitle><description>In a search for new cerebral protective agents with anti-anoxic (AA) and anti-lipid peroxidation (ALP) activities, a series of 4-arylpyrimidines, bearing an amino moiety in the C-5 position of the pyrimidine nucleus, was synthesized and tested for AA and ALP activities. Among them, 6-methyl-5-(4-methylpiperazin-1-ylcarbonyl)-4-(3-nitrophenyl )-2-phenylpyrimidin e (41, FK360) was most effective on both assays and on arachidonate-induced cerebral edema in rats. Structure-activity relationships in regard to AA activity of this series of compounds are also discussed.</description><subject>Animals</subject><subject>Chemistry</subject><subject>Exact sciences and technology</subject><subject>Heterocyclic compounds</subject><subject>Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings</subject><subject>Hypoxia, Brain - drug therapy</subject><subject>Lethal Dose 50</subject><subject>Lipid Peroxidation - drug effects</subject><subject>Mice</subject><subject>Mice, Inbred ICR</subject><subject>Organic chemistry</subject><subject>Preparations and properties</subject><subject>Pyrimidines - chemical synthesis</subject><subject>Pyrimidines - pharmacology</subject><subject>Pyrimidines - toxicity</subject><subject>Rats</subject><subject>Structure-Activity Relationship</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkElPwzAQhS0EgrKcOCP5wA2l2B47CzeEWCohOADnaGpPwCgkkR0K_QH8b1y1gtMs79M8zWPsWIqpVLo8t8N8qsVUaQVbbCJBF5lRCrbZRAhRZQpy2GP7Mb4LoYwoYJftSq1zyM2E_TyNn85T5H3HLQWaB2z5EPqR7OgXxPGVujFO-Wx2wR_6BbVcZxiW7bAM_sM73xF3FPwCV3TkX35849iNPsOu__Y29W49t37wjg8U0tolOvnhysKPyf2Q7TTYRjra1AP2cnP9fHWX3T_ezq4u7zMLICFTrqhU5RxhaV1hVZMbCShLqFA00pqyQGwklWSSWjSkyrmTlQPjrAMsKzhgZ-u7NvQxBmrqIb2R_qmlqFdZ1inLWot6lWWiT9b08Dn_IPfPrsNL-ulGx2ixbQJ21sc_TBudSwPwC4Slf5Q</recordid><startdate>1992</startdate><enddate>1992</enddate><creator>KUNO, A</creator><creator>SUGIYAMA, Y</creator><creator>KATSUTA, K</creator><creator>SAKAI, H</creator><creator>TAKASUGI, H</creator><general>Maruzen</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></search><sort><creationdate>1992</creationdate><title>Studies on cerebral protective agents. II: Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities</title><author>KUNO, A ; SUGIYAMA, Y ; KATSUTA, K ; SAKAI, H ; TAKASUGI, H</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3313-2d7929ddea8cd7c2f6513a1839a0f1c587aaf1e8e5d7c7fe28bd19d35dcd3a893</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1992</creationdate><topic>Animals</topic><topic>Chemistry</topic><topic>Exact sciences and technology</topic><topic>Heterocyclic compounds</topic><topic>Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings</topic><topic>Hypoxia, Brain - drug therapy</topic><topic>Lethal Dose 50</topic><topic>Lipid Peroxidation - drug effects</topic><topic>Mice</topic><topic>Mice, Inbred ICR</topic><topic>Organic chemistry</topic><topic>Preparations and properties</topic><topic>Pyrimidines - chemical synthesis</topic><topic>Pyrimidines - pharmacology</topic><topic>Pyrimidines - toxicity</topic><topic>Rats</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>KUNO, A</creatorcontrib><creatorcontrib>SUGIYAMA, Y</creatorcontrib><creatorcontrib>KATSUTA, K</creatorcontrib><creatorcontrib>SAKAI, H</creatorcontrib><creatorcontrib>TAKASUGI, H</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><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>KUNO, A</au><au>SUGIYAMA, Y</au><au>KATSUTA, K</au><au>SAKAI, H</au><au>TAKASUGI, H</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Studies on cerebral protective agents. II: Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem Pharm Bull (Tokyo)</addtitle><date>1992</date><risdate>1992</risdate><volume>40</volume><issue>9</issue><spage>2423</spage><epage>2431</epage><pages>2423-2431</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><coden>CPBTAL</coden><abstract>In a search for new cerebral protective agents with anti-anoxic (AA) and anti-lipid peroxidation (ALP) activities, a series of 4-arylpyrimidines, bearing an amino moiety in the C-5 position of the pyrimidine nucleus, was synthesized and tested for AA and ALP activities. Among them, 6-methyl-5-(4-methylpiperazin-1-ylcarbonyl)-4-(3-nitrophenyl )-2-phenylpyrimidin e (41, FK360) was most effective on both assays and on arachidonate-induced cerebral edema in rats. Structure-activity relationships in regard to AA activity of this series of compounds are also discussed.</abstract><cop>Tokyo</cop><pub>Maruzen</pub><pmid>1446365</pmid><doi>10.1248/cpb.40.2423</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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| identifier | ISSN: 0009-2363 |
| ispartof | Chemical & pharmaceutical bulletin, 1992, Vol.40 (9), p.2423-2431 |
| issn | 0009-2363 1347-5223 |
| language | eng |
| recordid | cdi_crossref_primary_10_1248_cpb_40_2423 |
| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Free Full-Text Journals in Chemistry |
| subjects | Animals Chemistry Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Hypoxia, Brain - drug therapy Lethal Dose 50 Lipid Peroxidation - drug effects Mice Mice, Inbred ICR Organic chemistry Preparations and properties Pyrimidines - chemical synthesis Pyrimidines - pharmacology Pyrimidines - toxicity Rats Structure-Activity Relationship |
| title | Studies on cerebral protective agents. II: Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities |
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