{"title":"新合成的曼尼希碱2-[(1,3-苯并噻唑-2-氨基)甲基]-5-甲基-2,4-二氢- 3h -吡唑-3-酮及其衍生物的体外抗炎活性","authors":"P. P. Rathi, V. More, V. Deshmukh, S. Chaudhari","doi":"10.33786/JCPR.2013.V03I04.001","DOIUrl":null,"url":null,"abstract":"The present study was aimed to synthesize a series 2-[(1,3-benzothiazol-2-ylamino)methyl]-5-methyl-2,4-dihydro-3 H -pyrazol-3-one (3 a-l) and to evaluate their in-vitro anti-inflammatory activity. The starting material (1a-l) was prepared by the application of cyclization reaction. In-vitro anti-inflammatory activity of synthesized compounds [3a-l] was evaluated using inhibition of bovine serum albumin denaturation method. 3c and 3l have shown significant in-vitro anti-inflammatory activity. The findings of present study clearly demonstrate that chloro functional group possess inhibition of bovine serum albumin denaturation capacity and has in-vitro anti-inflammatory activity. However methyl, methoxy and dimethyl derivatives show mild to moderate in-vitro anti-inflammatory activity.","PeriodicalId":23049,"journal":{"name":"The Pharma Research","volume":"10 1","pages":"30-40"},"PeriodicalIF":0.0000,"publicationDate":"2013-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"Invitro anti-inflammatory activity of newly synthesized mannich base 2-[(1,3-benzothiazol-2-ylamino)methyl]-5-methyl-2,4-dihydro-3H-pyrazol-3-one and its derivatives\",\"authors\":\"P. P. Rathi, V. More, V. Deshmukh, S. Chaudhari\",\"doi\":\"10.33786/JCPR.2013.V03I04.001\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The present study was aimed to synthesize a series 2-[(1,3-benzothiazol-2-ylamino)methyl]-5-methyl-2,4-dihydro-3 H -pyrazol-3-one (3 a-l) and to evaluate their in-vitro anti-inflammatory activity. The starting material (1a-l) was prepared by the application of cyclization reaction. In-vitro anti-inflammatory activity of synthesized compounds [3a-l] was evaluated using inhibition of bovine serum albumin denaturation method. 3c and 3l have shown significant in-vitro anti-inflammatory activity. The findings of present study clearly demonstrate that chloro functional group possess inhibition of bovine serum albumin denaturation capacity and has in-vitro anti-inflammatory activity. However methyl, methoxy and dimethyl derivatives show mild to moderate in-vitro anti-inflammatory activity.\",\"PeriodicalId\":23049,\"journal\":{\"name\":\"The Pharma Research\",\"volume\":\"10 1\",\"pages\":\"30-40\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2013-11-15\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"The Pharma Research\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.33786/JCPR.2013.V03I04.001\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"The Pharma Research","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.33786/JCPR.2013.V03I04.001","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 1
摘要
本研究旨在合成一系列2-[(1,3-苯并噻唑-2-氨基)甲基]-5-甲基-2,4-二氢-3 H -吡唑-3-酮(3 a- 1)并评价其体外抗炎活性。采用环化反应制备起始原料(1a-l)。采用抑制牛血清白蛋白变性法评价合成化合物[3a-l]的体外抗炎活性。3c和3l显示出显著的体外抗炎活性。本研究结果清楚地表明,氯官能团具有抑制牛血清白蛋白变性能力和体外抗炎活性。然而,甲基、甲氧基和二甲基衍生物显示轻度至中度的体外抗炎活性。
Invitro anti-inflammatory activity of newly synthesized mannich base 2-[(1,3-benzothiazol-2-ylamino)methyl]-5-methyl-2,4-dihydro-3H-pyrazol-3-one and its derivatives
The present study was aimed to synthesize a series 2-[(1,3-benzothiazol-2-ylamino)methyl]-5-methyl-2,4-dihydro-3 H -pyrazol-3-one (3 a-l) and to evaluate their in-vitro anti-inflammatory activity. The starting material (1a-l) was prepared by the application of cyclization reaction. In-vitro anti-inflammatory activity of synthesized compounds [3a-l] was evaluated using inhibition of bovine serum albumin denaturation method. 3c and 3l have shown significant in-vitro anti-inflammatory activity. The findings of present study clearly demonstrate that chloro functional group possess inhibition of bovine serum albumin denaturation capacity and has in-vitro anti-inflammatory activity. However methyl, methoxy and dimethyl derivatives show mild to moderate in-vitro anti-inflammatory activity.