首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis and antiviral activity of 1-(1,3-disubstitutedimidazolidyn-2-ylidene)-3-ethoxycarbonylmethylurea derivatives
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Synthesis and antiviral activity of 1-(1,3-disubstitutedimidazolidyn-2-ylidene)-3-ethoxycarbonylmethylurea derivatives

机译:1-(1,3-二取代咪唑啉基-2-亚烷基)-3-乙氧基羰基甲基脲衍生物的合成及抗病毒活性

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摘要

Novel 1-(1,3-disubstituted-imidazolidyn-2-ylidene)-3-ethoxycarbonylmethylurea derivatives (3a-3j) were obtained from appropriate 1-aryl-3-arylsulfonyl-1H-imidazolidine-2-imines (1a-1j) and ethyl isocyanatoacetate (2), which were subjected to condensation. Seven compounds were tested for their antiviral activity against HSV-1 and CVB3 viruses. Among the tested compounds, 3c was found to be active against HSV-1, proving that 4-methoxy substituent as R and 4-methyl substituent as R-1 are most beneficial for activity against this virus. Furthermore, 3e and 3g were active against CVB3, which demonstrated that both 4-methyl and 4-chloro substitution is tolerated as R-1, whereas 4-chloro and 2-methoxy substituents are best as R. It was also shown that the active compounds are characterized by relatively big surface area, small ovality, and greatest HOMO and LUMO energies in comparison to the rest of the compounds.
机译:从合适的1-芳基-3-芳基磺酰基-1H-咪唑烷-2-亚胺(1a-1j)获得了新的1-(1,3-二取代-咪唑啉基-2-亚甲基)-3-乙氧基羰基甲基脲衍生物(3a-3j)。和异氰酸根合乙酸乙酯(2)进行缩合。测试了七个化合物对HSV-1和CVB3病毒的抗病毒活性。在测试的化合物中,发现3c对HSV-1有活性,证明4-甲氧基取代基作为R和4-甲基取代基作为R-1对这种病毒的活性最有益。此外,3e和3g对CVB3具有活性,这表明4-甲基和4-氯取代均被耐受为R-1,而4-氯和2-甲氧基取代基为R最好。与其余化合物相比,这些化合物的特征是具有较大的表面积,较小的椭圆度以及最大的HOMO和LUMO能量。

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