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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >COX-2 inhibitory and GABAergic activity of newly synthesized 2(3H)-furanone
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COX-2 inhibitory and GABAergic activity of newly synthesized 2(3H)-furanone

机译：新合成的2（3H）-呋喃酮的COX-2抑制和GABA能活性

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A series of 5-(substituted-phenyl)-3-(substituted-arylidene)-2(3H)-furanones were synthesized by two step process. Molecular docking experiments were carried out to identify potential COX-2 inhibitor and GABA modulator among all synthesized furanone derivatives. Elemental analysis values were found within ±0.4% of the theoretical values. The IR spectra of compounds were recorded in KBr on Perkin Elmer BX-II FTIR spectrophotometer. The proton magnetic resonance spectra (1H NMR) were recorded on Bruker 300MHz instrument in CDCl3 using tetramethylsilane [(CH3)4Si] (TMS) as internal standard. All Synthesized furanones were screened for anti-inflammatory activity by Carrageenin induced rat paw edema method and by PTZ induced seizure method for anticonvulsant activity. Result indicate that tested compounds 5- (4-chloro-3methyl-phenyl)-3-(4-dimethylamino-benzylidene)-3Hfuran-2-one (15) and 3- Anthracen-9-ylmethylene-5-(4-chloro-3-methyl-phenyl)-3H-furan-2-one (16) possess the strongest anti-inflammatory activity, comparable to that of indomethacin, and the compound 16 also exhibits GABA modulator activity less comparable to diazepam.
机译：通过两步法合成了一系列5-（取代苯基）-3-（取代亚芳基）-2（3H）-呋喃酮。进行了分子对接实验，以在所有合成的呋喃酮衍生物中鉴定潜在的COX-2抑制剂和GABA调节剂。元素分析值在理论值的±0.4％之内。化合物的红外光谱在Perkin Elmer BX-II FTIR分光光度计上以KBr记录。使用四甲基硅烷[（CH3）4Si]（TMS）作为内标，在CD300中的Bruker 300MHz仪器上记录质子磁共振谱（1H NMR）。通过角叉菜胶诱导的大鼠爪水肿方法和PTZ诱导的癫痫发作方法筛选所有合成的呋喃酮的抗炎活性。结果表明所测试的化合物5-（4-氯-3甲基-苯基）-3-（4-二甲基氨基-亚苄基）-3H呋喃-2-酮（15）和3-蒽-9-基亚甲基-5-（4-氯（-3-甲基-苯基）-3H-呋喃-2-酮（16）具有最强的消炎活性，可与消炎痛相媲美，化合物16的GABA调节剂活性也比地西epa低。

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