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4,4'-(芳基亚甲基)双(1H-吡唑-5-醇)对小反刍兽疫病毒(PPRV)的合成及抗病毒活性

Synthesis and antiviral activity of 4,4'-(arylmethylene)bis(1H-pyrazol-5-ols) against peste des petits ruminant virus (PPRV).

作者信息

Sujatha Kuppusamy, Shanthi Gnanamani, Selvam Nagarajan Panneer, Manoharan Seeralan, Perumal Paramasivan T, Rajendran Melani

机构信息

Sri Ramachandra College of Pharmacy, Sri Ramachandra University, Porur, Chennai 600 116, India.

出版信息

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4501-3. doi: 10.1016/j.bmcl.2009.02.113. Epub 2009 Mar 3.

Abstract

An efficient and eco-friendly method for the synthesis of 4,4'-(arylmethylene)bis(1H-pyrazol-5-ols) has been accomplished by tandem Knoevenagel-Michael reaction of two equivalents of 5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one with various aromatic aldehydes catalyzed by ceric ammonium nitrate (CAN) in water. All the synthesized compounds 3a-j were evaluated for in vitro antiviral activity against peste des petits ruminant virus (PPRV). Compound 3i emerged as the most interesting compound in this series exhibiting excellent antiviral activity against PPRV and found to be more potent than the standard drug ribavirin used.

摘要

通过硝酸铈铵(CAN)催化两当量的5-甲基-2-苯基-2,4-二氢-3H-吡唑-3-酮与各种芳香醛在水中进行串联Knoevenagel-Michael反应,实现了一种高效且环保的合成4,4'-(芳基亚甲基)双(1H-吡唑-5-醇)的方法。对所有合成的化合物3a-j进行了抗小反刍兽疫病毒(PPRV)的体外抗病毒活性评估。化合物3i是该系列中最具吸引力的化合物,对PPRV表现出优异的抗病毒活性,且发现其比所用的标准药物利巴韦林更有效。

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