Vasorelaxant activity of phthalazinones and related compounds
The vasorelaxant activity of some dihydrostilbenamides, imidazo[2,1-a]isoindoles, pyrimido[2,1-a]isoindoles and phthalazinones has been evaluated. Three phthalazinones reverted the 10μM phenylephrine induced contraction with EC50
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (10), p.2786-2790 |
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| container_issue | 10 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 16 |
| creator | Olmo, Esther del Barboza, Bianca Ybarra, Ma Inés López-Pérez, José Luis Carrón, Rosalía Sevilla, Ma Angeles Boselli, Cinthia Feliciano, Arturo San |
| description | The vasorelaxant activity of some dihydrostilbenamides, imidazo[2,1-a]isoindoles, pyrimido[2,1-a]isoindoles and phthalazinones has been evaluated. Three phthalazinones reverted the 10μM phenylephrine induced contraction with EC50 |
| doi_str_mv | 10.1016/j.bmcl.2006.02.003 |
| format | Article |
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Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10−5M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50=0.43μM) the affinities for α1A, α1B and α1D adrenergic sub-receptors were determined.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2006.02.003</identifier><identifier>PMID: 16513345</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Animals ; Biological and medical sciences ; Cardiovascular system ; Dihydrostilbenamide ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Phthalazines - chemistry ; Phthalazines - pharmacology ; Phthalazinone ; Rat aorta rings ; Rats ; Rats, Wistar ; Receptors, Adrenergic, alpha - classification ; Receptors, Adrenergic, alpha - drug effects ; Vas Deferens - drug effects ; Vas Deferens - physiology ; Vasodilation - drug effects ; Vasodilator agents. Cerebral vasodilators ; Vasorelaxant activity ; α1A, α1B and α1D sub-receptors affinity</subject><ispartof>Bioorganic & medicinal chemistry letters, 2006-05, Vol.16 (10), p.2786-2790</ispartof><rights>2006 Elsevier Ltd</rights><rights>2006 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-efe0371a9e494eb29510122f1dfcc2472ecc466b5abf5862c6d72f6ce02aef943</citedby><cites>FETCH-LOGICAL-c415t-efe0371a9e494eb29510122f1dfcc2472ecc466b5abf5862c6d72f6ce02aef943</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X06001752$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=17642469$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16513345$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Olmo, Esther del</creatorcontrib><creatorcontrib>Barboza, Bianca</creatorcontrib><creatorcontrib>Ybarra, Ma Inés</creatorcontrib><creatorcontrib>López-Pérez, José Luis</creatorcontrib><creatorcontrib>Carrón, Rosalía</creatorcontrib><creatorcontrib>Sevilla, Ma Angeles</creatorcontrib><creatorcontrib>Boselli, Cinthia</creatorcontrib><creatorcontrib>Feliciano, Arturo San</creatorcontrib><title>Vasorelaxant activity of phthalazinones and related compounds</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>The vasorelaxant activity of some dihydrostilbenamides, imidazo[2,1-a]isoindoles, pyrimido[2,1-a]isoindoles and phthalazinones has been evaluated. Three phthalazinones reverted the 10μM phenylephrine induced contraction with EC50<1μM. The affinities of compound 9h for α1A, α1B and α1D adrenergic sub-receptors have been determined.
Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10−5M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50=0.43μM) the affinities for α1A, α1B and α1D adrenergic sub-receptors were determined.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cardiovascular system</subject><subject>Dihydrostilbenamide</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Phthalazines - chemistry</subject><subject>Phthalazines - pharmacology</subject><subject>Phthalazinone</subject><subject>Rat aorta rings</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Adrenergic, alpha - classification</subject><subject>Receptors, Adrenergic, alpha - drug effects</subject><subject>Vas Deferens - drug effects</subject><subject>Vas Deferens - physiology</subject><subject>Vasodilation - drug effects</subject><subject>Vasodilator agents. Cerebral vasodilators</subject><subject>Vasorelaxant activity</subject><subject>α1A, α1B and α1D sub-receptors affinity</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0E2L1EAQgOFGFHdc_QMeJBe9JVZ1Kp0J6GFZ_IIFLyremk6lmu0hSY_dmcX115thBvamp7o8VRSvUi8RKgQ0b3dVP_FYaQBTga4A6kdqg2SorAmax2oDnYFy29HPC_Us5x0AEhA9VRdoGqxrajbq_Q-XY5LR_XbzUjhewl1Y7ovoi_3tcutG9yfMcZZcuHkojm6RoeA47eNhHvJz9cS7McuL87xU3z9--Hb9ubz5-unL9dVNyYTNUooXqFt0nVBH0uuuWf_X2uPgmTW1WpjJmL5xvW-2RrMZWu0NC2gnvqP6Ur053d2n-OsgebFTyCzj6GaJh2xNu0WkLf4XYotNi229Qn2CnGLOSbzdpzC5dG8R7LGu3dljXXusa0Hbte669Op8_dBPMjysnHOu4PUZuMxu9MnNHPKDaw1pMt3q3p2crNHugiSbOcjMMoQkvNghhn_98Rdpnph-</recordid><startdate>20060515</startdate><enddate>20060515</enddate><creator>Olmo, Esther del</creator><creator>Barboza, Bianca</creator><creator>Ybarra, Ma Inés</creator><creator>López-Pérez, José Luis</creator><creator>Carrón, Rosalía</creator><creator>Sevilla, Ma Angeles</creator><creator>Boselli, Cinthia</creator><creator>Feliciano, Arturo San</creator><general>Elsevier Ltd</general><general>Elsevier</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20060515</creationdate><title>Vasorelaxant activity of phthalazinones and related compounds</title><author>Olmo, Esther del ; Barboza, Bianca ; Ybarra, Ma Inés ; López-Pérez, José Luis ; Carrón, Rosalía ; Sevilla, Ma Angeles ; Boselli, Cinthia ; Feliciano, Arturo San</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c415t-efe0371a9e494eb29510122f1dfcc2472ecc466b5abf5862c6d72f6ce02aef943</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cardiovascular system</topic><topic>Dihydrostilbenamide</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Phthalazines - chemistry</topic><topic>Phthalazines - pharmacology</topic><topic>Phthalazinone</topic><topic>Rat aorta rings</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Adrenergic, alpha - classification</topic><topic>Receptors, Adrenergic, alpha - drug effects</topic><topic>Vas Deferens - drug effects</topic><topic>Vas Deferens - physiology</topic><topic>Vasodilation - drug effects</topic><topic>Vasodilator agents. 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Three phthalazinones reverted the 10μM phenylephrine induced contraction with EC50<1μM. The affinities of compound 9h for α1A, α1B and α1D adrenergic sub-receptors have been determined.
Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10−5M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50=0.43μM) the affinities for α1A, α1B and α1D adrenergic sub-receptors were determined.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>16513345</pmid><doi>10.1016/j.bmcl.2006.02.003</doi><tpages>5</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2006-05, Vol.16 (10), p.2786-2790 |
| issn | 0960-894X 1464-3405 |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Biological and medical sciences Cardiovascular system Dihydrostilbenamide Male Medical sciences Pharmacology. Drug treatments Phthalazines - chemistry Phthalazines - pharmacology Phthalazinone Rat aorta rings Rats Rats, Wistar Receptors, Adrenergic, alpha - classification Receptors, Adrenergic, alpha - drug effects Vas Deferens - drug effects Vas Deferens - physiology Vasodilation - drug effects Vasodilator agents. Cerebral vasodilators Vasorelaxant activity α1A, α1B and α1D sub-receptors affinity |
| title | Vasorelaxant activity of phthalazinones and related compounds |
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