新型吡唑取代的不同含氮杂环体系作为潜在抗炎剂的设计与合成
Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents.
作者信息
Nossier Eman S, Fahmy Hoda H, Khalifa Nagy M, El-Eraky Wafaa I, Baset Marawan A
机构信息
Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt.
Department of Therapeutical Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza 12622, Egypt.
出版信息
Molecules. 2017 Mar 24;22(4):512. doi: 10.3390/molecules22040512.
Abstract
With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.
摘要
为了开发新型抗炎支架，通过不同的化学反应合成了一系列新的在C-4位带有吡唑取代的各种含氮杂环系统，并通过光谱和元素数据进行了验证。使用角叉菜胶诱导的爪肿胀标准技术对新得到的化合物进行了抗炎活性研究，结果表明，化合物的水肿抑制率分别为85.23±1.92和85.78±0.99，显示出增强的效力，高于标准参考药物吲哚美辛和塞来昔布（分别为72.99%和83.76%）。在此开展了分子模拟研究，以验证所获得的药理数据，并为观察到的抗炎行为提供合理的证据。
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