Michael G Kallitsakis, Angelo Carotti, Marco Catto, Aikaterini Peperidou, Dimitra J Hadjipavlou-Litina, Konstantinos E Litinas
{"title":"含有嘌呤、香豆素和异恶唑啉或异恶唑基团的新型杂化分子的合成及生物学评价。","authors":"Michael G Kallitsakis, Angelo Carotti, Marco Catto, Aikaterini Peperidou, Dimitra J Hadjipavlou-Litina, Konstantinos E Litinas","doi":"10.2174/1874104501711010196","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>The 1,3-dipolar cycloaddition reactions of nitrile oxides formed <i>in situ</i> (in the presence of NCS and Et<sub>3</sub>N) from the oximes of (purin-9-yl)acetaldehyde or (coumarinyloxy)acetaldehyde with allyloxycoumarins or 9-allylpurines, respectively resulted in 3,5-disubstituted isoxazolines. The similar reactions of propargyloxycoumarins or 9-propargylpurines led to 3,5-disubstituted isoxazoles by treatment with PIDA and catalytic amount of TFA.</p><p><strong>Methods: </strong>The new compounds were tested <i>in vitro</i> as antioxidant agents and inhibitors of soybean lipoxygenase LO, AChE and MAO-B.</p><p><strong>Results: </strong>The majority of the compounds showed significant hydroxyl radical scavenging activity. Compounds <b>4k</b> and <b>4n</b> presented LO inhibitory activity.</p><p><strong>Conclusion: </strong>Compound <b>13</b>e presents an antioxidant significant profile combining anti-LO, anti-AChE and anti-MAO-B activities.</p>","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"11 ","pages":"196-211"},"PeriodicalIF":0.0000,"publicationDate":"2017-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1874104501711010196","citationCount":"11","resultStr":"{\"title\":\"Synthesis and Biological Evaluation of Novel Hybrid Molecules Containing Purine, Coumarin and Isoxazoline or Isoxazole Moieties.\",\"authors\":\"Michael G Kallitsakis, Angelo Carotti, Marco Catto, Aikaterini Peperidou, Dimitra J Hadjipavlou-Litina, Konstantinos E Litinas\",\"doi\":\"10.2174/1874104501711010196\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>The 1,3-dipolar cycloaddition reactions of nitrile oxides formed <i>in situ</i> (in the presence of NCS and Et<sub>3</sub>N) from the oximes of (purin-9-yl)acetaldehyde or (coumarinyloxy)acetaldehyde with allyloxycoumarins or 9-allylpurines, respectively resulted in 3,5-disubstituted isoxazolines. The similar reactions of propargyloxycoumarins or 9-propargylpurines led to 3,5-disubstituted isoxazoles by treatment with PIDA and catalytic amount of TFA.</p><p><strong>Methods: </strong>The new compounds were tested <i>in vitro</i> as antioxidant agents and inhibitors of soybean lipoxygenase LO, AChE and MAO-B.</p><p><strong>Results: </strong>The majority of the compounds showed significant hydroxyl radical scavenging activity. Compounds <b>4k</b> and <b>4n</b> presented LO inhibitory activity.</p><p><strong>Conclusion: </strong>Compound <b>13</b>e presents an antioxidant significant profile combining anti-LO, anti-AChE and anti-MAO-B activities.</p>\",\"PeriodicalId\":39133,\"journal\":{\"name\":\"Open Medicinal Chemistry Journal\",\"volume\":\"11 \",\"pages\":\"196-211\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2017-11-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.2174/1874104501711010196\",\"citationCount\":\"11\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Open Medicinal Chemistry Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1874104501711010196\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2017/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q2\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Open Medicinal Chemistry Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1874104501711010196","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2017/1/1 0:00:00","PubModel":"eCollection","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
Synthesis and Biological Evaluation of Novel Hybrid Molecules Containing Purine, Coumarin and Isoxazoline or Isoxazole Moieties.
Introduction: The 1,3-dipolar cycloaddition reactions of nitrile oxides formed in situ (in the presence of NCS and Et3N) from the oximes of (purin-9-yl)acetaldehyde or (coumarinyloxy)acetaldehyde with allyloxycoumarins or 9-allylpurines, respectively resulted in 3,5-disubstituted isoxazolines. The similar reactions of propargyloxycoumarins or 9-propargylpurines led to 3,5-disubstituted isoxazoles by treatment with PIDA and catalytic amount of TFA.
Methods: The new compounds were tested in vitro as antioxidant agents and inhibitors of soybean lipoxygenase LO, AChE and MAO-B.
Results: The majority of the compounds showed significant hydroxyl radical scavenging activity. Compounds 4k and 4n presented LO inhibitory activity.
Conclusion: Compound 13e presents an antioxidant significant profile combining anti-LO, anti-AChE and anti-MAO-B activities.
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