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

P. P. Rathi, V. More, V. Deshmukh, S. Chaudhari
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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。
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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.
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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
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