Design, Synthesis, Characterisation and Pharmacological Evaluation of Some Novel Substituted Pyrimidine 2-one Derivatives

S. Gejalakshmi, N. Harikrishnan
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Abstract

2,3-dihydropyrimidin-2(1H)-one derivatives were known to undergo cyclo-condensation of benzaldehyde, urea and ethyl acetoacetate and evaluate their antioxidant and in vitro anti-inflammatory activity. Dihydropyrimidinones are mainly synthesized by Biginelli reaction, which involves cyclo condensation of benzaldehyde, urea and ethyl acetoacetate. The prepared compounds were characterized by noting their melting point, thin layer chromatography ultraviolet spectroscopy, infrared spectroscopy, nuclear magnetic resonance and Mass spectroscopy and were scrutinized for its in vitro anti-inflammatory activity and antioxidant activity by in vitro cell culture studies. The melting point, thin layer chromatography and ultraviolet spectroscopy of the synthesized compounds were found to be pure and identified chemically. The molecular structure and molecular mass of compounds were confirmed by Infrared, nuclear magnetic resonance and Mass spectroscopy. The IC50 value of compound 1 and compound 2 by hydrogen peroxide method was found to be 30.25 μg/ml and 26.06 μg/ml respectively. The IC50 value of compound 1 and compound 2 by DPPH assay method was found to be 27.872 μg/ml and 25.467 μg/ml respectively. Synthesized compounds also show anti-inflammatory activity. The result obtained in this research work is clearly indicating that the synthesized molecules possess both antioxidant activity and anti-inflammatory activity.
一些新型取代嘧啶2- 1衍生物的设计、合成、表征及药理评价
2,3-二氢嘧啶-2(1H)- 1衍生物经苯甲醛、尿素和乙酰乙酸乙酯的环缩合反应,并评价了其抗氧化和体外抗炎活性。双氢嘧啶类化合物主要通过苯甲醛、尿素和乙酰乙酸乙酯的Biginelli反应合成。采用熔点、薄层色谱、紫外光谱、红外光谱、核磁共振和质谱等方法对化合物进行了表征,并通过体外细胞培养研究了化合物的体外抗炎活性和抗氧化活性。经熔点、薄层色谱和紫外光谱分析,合成的化合物纯度较高,经化学鉴定。通过红外光谱、核磁共振和质谱等手段确定了化合物的分子结构和分子质量。双氧水法测定化合物1和化合物2的IC50值分别为30.25 μg/ml和26.06 μg/ml。DPPH法测定化合物1和化合物2的IC50值分别为27.872和25.467 μg/ml。合成的化合物也显示出抗炎活性。本研究结果清楚地表明所合成的分子具有抗氧化和抗炎活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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