2-氨基-4,5-二苯基-1-(取代)- 1h -吡咯-3-碳腈衍生物的合成及抗炎活性

S. Dholakia
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引用次数: 1

摘要

吡咯是一种特殊的活性杂环化合物,具有多种药理活性,特别是作为抗炎、抗疟疾、抗菌、抗病毒、抗结核和酶抑制药物的有前途的支架。为了探索这种支架,我们合成了一系列2-氨基-4,5-二苯基-1-(取代)- 1h -吡咯-3-碳腈,并对其进行了抗炎活性筛选。用1H核磁共振、质谱和傅里叶转移红外光谱对合成的新化合物进行了结构表征。所有化合物均采用大鼠足部水肿法筛选抗炎活性。其中,化合物1e表现出比标准药物依托妥昔布更强的活性,在3 h和5 h时对足跖水肿的抑制作用最高。
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Synthesis and anti-inflammatory activity of 2-amino-4,5-diphenyl-1-(substituted)-1H-pyrrole-3- carbonitrile derivatives
Pyrrole is privileged and active heterocycle with diverse pharmacological activities that specifically serve as a promising scaffold for antiinflammatory, antimalarial, antimicrobial, antiviral, antitubercular, and enzyme-inhibiting drugs. In an attempt to explore this scaffold, a series of 2- amino-4,5-diphenyl-1-(substituted)-1H-pyrrole-3-carbonitrilewere synthesized and screened for anti-inflammatory activity. The structures of synthesized novel compounds were characterized by 1H Nuclear Magnetic Resonance, Mass and Fourier Transfer Infrared spectroscopic data. All the compounds are screened for anti-inflammatory activity using the rat paw edema method. Among all, compound 1e exhibited more potent activity than the standard drug etoricoxib with the highest inhibition in paw edema at 3 h and 5 h.
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