Benzylpiperazine Derivatives. I. Syntheses and Biological Activities of 1(2, 3, 4-Trimethoxybenzyl) piperazine Derivatives
A series of 1- (2, 3, 4-trimethoxybenzyl) piperazine (trimetazidine) derivatives were prepared and tested for cerebral vasodilating activity. Almost all the compounds possess stronger activity than trimetazidine and among them, the γ-amino tertiary alcohols 6e-j exhibit potent cerebral vasodilating...
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| Veröffentlicht in: | Chemical & pharmaceutical bulletin 1987/07/25, Vol.35(7), pp.2774-2781 |
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| container_issue | 7 |
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| container_title | Chemical & pharmaceutical bulletin |
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| creator | OHTAKA, HIROSHI MIYAKE, MUTSUO KANAZAWA, TOSHIRO ITO, KEIZO TSUKAMOTO, GORO |
| description | A series of 1- (2, 3, 4-trimethoxybenzyl) piperazine (trimetazidine) derivatives were prepared and tested for cerebral vasodilating activity. Almost all the compounds possess stronger activity than trimetazidine and among them, the γ-amino tertiary alcohols 6e-j exhibit potent cerebral vasodilating activities which are superior to those of cinnarizine and papaverine. Moreover, these compounds show a selective vasodilating effect on vertebral arteries. |
| doi_str_mv | 10.1248/cpb.35.2774 |
| format | Article |
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I. Syntheses and Biological Activities of 1(2, 3, 4-Trimethoxybenzyl) piperazine Derivatives</title><title>Chemical & pharmaceutical bulletin</title><addtitle>Chem. Pharm. Bull.</addtitle><description>A series of 1- (2, 3, 4-trimethoxybenzyl) piperazine (trimetazidine) derivatives were prepared and tested for cerebral vasodilating activity. Almost all the compounds possess stronger activity than trimetazidine and among them, the γ-amino tertiary alcohols 6e-j exhibit potent cerebral vasodilating activities which are superior to those of cinnarizine and papaverine. Moreover, these compounds show a selective vasodilating effect on vertebral arteries.</description><subject>Animals</subject><subject>Benzyl Compounds - chemical synthesis</subject><subject>Benzyl Compounds - pharmacology</subject><subject>cerebral vasodilator</subject><subject>Cerebrovascular Circulation - drug effects</subject><subject>Chemical Phenomena</subject><subject>Chemistry</subject><subject>Dogs</subject><subject>Exact sciences and technology</subject><subject>Female</subject><subject>Grignard reaction</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>Male</subject><subject>Mannich reaction</subject><subject>Organic chemistry</subject><subject>piperazine</subject><subject>Piperazines - chemical synthesis</subject><subject>Piperazines - pharmacology</subject><subject>Preparations and properties</subject><subject>trimetazidine</subject><subject>Vasodilator Agents - chemical synthesis</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkUtr3DAUhUVpSSdpV1kHBAmlpbGjp2Ut8-gjEOiiyVrI8nVGg8d2JE_ozK-P3BmmEKqFBDof50j3IHRMSU6ZKC_cUOVc5kwp8QbNKBcqk4zxt2hGCNEZ4wV_jw5jXBDCJFH8AB3wQinGyhnaXEG3WbeDHyDYje8A30Dwz3b0zxBzfJvj3-tunEOEiG1X4yvft_2jd7bFly5BfvRJ6RtMP7NzzM-xyO6DX8I47_-sq7_eX_D_3T-gd41tI3zcnUfo4fu3--uf2d2vH7fXl3eZk5KITEJJZS0EZYXTWitLSFXXFqywrKaCV8C1kE4o1XANVboDWvGS1YJQqyvGj9Cnre8Q-qcVxNEsfXTQtraDfhVNSdNKc0zg6Stw0a9Cl95mqCgIFUoXKlFft5QLfYwBGjOkD9uwNpSYycekPgyXZuoj0Sc7z1W1hHrP7gpI-tlOtzENtQm2cz7usZJLysmE3WyxRRztI-x1G0bvWpgiqZblFKu225T-T57bYKDjL6KTqgI</recordid><startdate>1987</startdate><enddate>1987</enddate><creator>OHTAKA, HIROSHI</creator><creator>MIYAKE, MUTSUO</creator><creator>KANAZAWA, TOSHIRO</creator><creator>ITO, KEIZO</creator><creator>TSUKAMOTO, GORO</creator><general>The Pharmaceutical Society of Japan</general><general>Maruzen</general><general>Japan Science and Technology Agency</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>7TK</scope><scope>7TM</scope><scope>7U9</scope><scope>H94</scope><scope>7X8</scope></search><sort><creationdate>1987</creationdate><title>Benzylpiperazine Derivatives. I. Syntheses and Biological Activities of 1(2, 3, 4-Trimethoxybenzyl) piperazine Derivatives</title><author>OHTAKA, HIROSHI ; MIYAKE, MUTSUO ; KANAZAWA, TOSHIRO ; ITO, KEIZO ; TSUKAMOTO, GORO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5504-5e815d44126c9997a00bddaea4a2d143be3945c477f39eb2d1e1b382d401a9b23</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Animals</topic><topic>Benzyl Compounds - chemical synthesis</topic><topic>Benzyl Compounds - pharmacology</topic><topic>cerebral vasodilator</topic><topic>Cerebrovascular Circulation - drug effects</topic><topic>Chemical Phenomena</topic><topic>Chemistry</topic><topic>Dogs</topic><topic>Exact sciences and technology</topic><topic>Female</topic><topic>Grignard reaction</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>Male</topic><topic>Mannich reaction</topic><topic>Organic chemistry</topic><topic>piperazine</topic><topic>Piperazines - chemical synthesis</topic><topic>Piperazines - pharmacology</topic><topic>Preparations and properties</topic><topic>trimetazidine</topic><topic>Vasodilator Agents - chemical synthesis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>OHTAKA, HIROSHI</creatorcontrib><creatorcontrib>MIYAKE, MUTSUO</creatorcontrib><creatorcontrib>KANAZAWA, TOSHIRO</creatorcontrib><creatorcontrib>ITO, KEIZO</creatorcontrib><creatorcontrib>TSUKAMOTO, GORO</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>Neurosciences Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>OHTAKA, HIROSHI</au><au>MIYAKE, MUTSUO</au><au>KANAZAWA, TOSHIRO</au><au>ITO, KEIZO</au><au>TSUKAMOTO, GORO</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Benzylpiperazine Derivatives. I. Syntheses and Biological Activities of 1(2, 3, 4-Trimethoxybenzyl) piperazine Derivatives</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem. Pharm. Bull.</addtitle><date>1987</date><risdate>1987</risdate><volume>35</volume><issue>7</issue><spage>2774</spage><epage>2781</epage><pages>2774-2781</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><coden>CPBTAL</coden><abstract>A series of 1- (2, 3, 4-trimethoxybenzyl) piperazine (trimetazidine) derivatives were prepared and tested for cerebral vasodilating activity. Almost all the compounds possess stronger activity than trimetazidine and among them, the γ-amino tertiary alcohols 6e-j exhibit potent cerebral vasodilating activities which are superior to those of cinnarizine and papaverine. 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| ispartof | Chemical and Pharmaceutical Bulletin, 1987/07/25, Vol.35(7), pp.2774-2781 |
| issn | 0009-2363 1347-5223 |
| language | eng |
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| source | J-STAGE Free; MEDLINE; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Animals Benzyl Compounds - chemical synthesis Benzyl Compounds - pharmacology cerebral vasodilator Cerebrovascular Circulation - drug effects Chemical Phenomena Chemistry Dogs Exact sciences and technology Female Grignard reaction Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Male Mannich reaction Organic chemistry piperazine Piperazines - chemical synthesis Piperazines - pharmacology Preparations and properties trimetazidine Vasodilator Agents - chemical synthesis |
| title | Benzylpiperazine Derivatives. I. Syntheses and Biological Activities of 1(2, 3, 4-Trimethoxybenzyl) piperazine Derivatives |
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