Kikkeri N. Mohana , Basavapatna N. Prasanna Kumar , Lingappa Mallesha
{"title":"一些嘧啶衍生物的合成及其生物活性","authors":"Kikkeri N. Mohana , Basavapatna N. Prasanna Kumar , Lingappa Mallesha","doi":"10.1016/j.dit.2013.08.004","DOIUrl":null,"url":null,"abstract":"<div><h3>Objectives</h3><p>To synthesize a variety of pyrimidine analogs, <strong>3</strong>, <strong>4</strong>, <strong>5</strong>, <strong>6(a–d)</strong>, <strong>7(a–d)</strong> and their anticonvulsant and antioxidant activity was determined.</p></div><div><h3>Methods</h3><p>Using 5-bromo-2,4-dichloropyrimidine and hydrazine hydrate, new compounds were synthesized. The structures of all the new compounds are established on the basis of FT-IR, <sup>1</sup>H NMR and mass spectral data. Anticonvulsant study was done by MES seizure model and rotorod method was employed to determine the neurotoxicity. Antioxidant activity was done by DPPH method.</p></div><div><h3>Results</h3><p>All the compounds were synthesized in good yield. Among the new compounds, <strong>6c</strong> and <strong>7c</strong> are found to be most potent and showed no neurotoxicity. All the compounds showed DPPH radical scavenging activity, where compounds <strong>7b</strong>, <strong>7a</strong> and <strong>6b</strong> were the best radical scavengers.</p></div><div><h3>Conclusions</h3><p>The results obtained justify the usage of these compounds from their promising anticonvulsant and antioxidant activity. Therefore, the nature of groups is very important for anticonvulsant activity in MES model.</p></div>","PeriodicalId":11284,"journal":{"name":"Drug Invention Today","volume":"5 3","pages":"Pages 216-222"},"PeriodicalIF":0.0000,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.dit.2013.08.004","citationCount":"58","resultStr":"{\"title\":\"Synthesis and biological activity of some pyrimidine derivatives\",\"authors\":\"Kikkeri N. Mohana , Basavapatna N. Prasanna Kumar , Lingappa Mallesha\",\"doi\":\"10.1016/j.dit.2013.08.004\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Objectives</h3><p>To synthesize a variety of pyrimidine analogs, <strong>3</strong>, <strong>4</strong>, <strong>5</strong>, <strong>6(a–d)</strong>, <strong>7(a–d)</strong> and their anticonvulsant and antioxidant activity was determined.</p></div><div><h3>Methods</h3><p>Using 5-bromo-2,4-dichloropyrimidine and hydrazine hydrate, new compounds were synthesized. The structures of all the new compounds are established on the basis of FT-IR, <sup>1</sup>H NMR and mass spectral data. Anticonvulsant study was done by MES seizure model and rotorod method was employed to determine the neurotoxicity. Antioxidant activity was done by DPPH method.</p></div><div><h3>Results</h3><p>All the compounds were synthesized in good yield. Among the new compounds, <strong>6c</strong> and <strong>7c</strong> are found to be most potent and showed no neurotoxicity. All the compounds showed DPPH radical scavenging activity, where compounds <strong>7b</strong>, <strong>7a</strong> and <strong>6b</strong> were the best radical scavengers.</p></div><div><h3>Conclusions</h3><p>The results obtained justify the usage of these compounds from their promising anticonvulsant and antioxidant activity. Therefore, the nature of groups is very important for anticonvulsant activity in MES model.</p></div>\",\"PeriodicalId\":11284,\"journal\":{\"name\":\"Drug Invention Today\",\"volume\":\"5 3\",\"pages\":\"Pages 216-222\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2013-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/j.dit.2013.08.004\",\"citationCount\":\"58\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Invention Today\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0975761913000641\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Invention Today","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0975761913000641","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and biological activity of some pyrimidine derivatives
Objectives
To synthesize a variety of pyrimidine analogs, 3, 4, 5, 6(a–d), 7(a–d) and their anticonvulsant and antioxidant activity was determined.
Methods
Using 5-bromo-2,4-dichloropyrimidine and hydrazine hydrate, new compounds were synthesized. The structures of all the new compounds are established on the basis of FT-IR, 1H NMR and mass spectral data. Anticonvulsant study was done by MES seizure model and rotorod method was employed to determine the neurotoxicity. Antioxidant activity was done by DPPH method.
Results
All the compounds were synthesized in good yield. Among the new compounds, 6c and 7c are found to be most potent and showed no neurotoxicity. All the compounds showed DPPH radical scavenging activity, where compounds 7b, 7a and 6b were the best radical scavengers.
Conclusions
The results obtained justify the usage of these compounds from their promising anticonvulsant and antioxidant activity. Therefore, the nature of groups is very important for anticonvulsant activity in MES model.