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通过Sydnones与炔酮的1,3-偶极环加成反应便捷合成含5-硝基噻吩部分的1,3,4-三取代吡唑及其抗菌活性评价

Convenient access to 1,3,4-trisubstituted pyrazoles carrying 5-nitrothiophene moiety via 1,3-dipolar cycloaddition of sydnones with acetylenic ketones and their antimicrobial evaluation.

作者信息

Rai N Satheesha, Kalluraya Balakrishna, Lingappa B, Shenoy Shaliny, Puranic Vedavati G

机构信息

Department of Post-Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangothri-574 199, Karnataka, India.

出版信息

Eur J Med Chem. 2008 Aug;43(8):1715-20. doi: 10.1016/j.ejmech.2007.08.002. Epub 2007 Aug 30.

Abstract

Novel 1-aryl-3-(5-nitro-2-thienyl)-4-aroyl-pyrazoles 7 have been synthesized by the 1,3-dipolar cycloaddition of 3-arylsydnones 3 with 1-aryl-3-(5-nitro-2-thienyl)-2-propyn-1-ones 6. The newly synthesized compounds were well characterized by elemental analysis, IR, (1)H NMR and mass spectral studies. They were also screened for their antibacterial and antifungal activities against a variety of microorganisms and the results of such studies have been discussed in this article.

摘要

通过3-芳基斯德酮3与1-芳基-3-(5-硝基-2-噻吩基)-2-丙炔-1-酮6的1,3-偶极环加成反应合成了新型1-芳基-3-(5-硝基-2-噻吩基)-4-芳酰基吡唑7。通过元素分析、红外光谱、核磁共振氢谱和质谱研究对新合成的化合物进行了充分表征。还对它们针对多种微生物的抗菌和抗真菌活性进行了筛选,本文讨论了这些研究结果。

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