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Synthesis, anti-tuberculosis and anti-bacterial activities of sulfonamide bearing 4-((2-(5-bromo-1H-pyrazolo[3,4-b]pyridin-1-yl)-2-oxoethyl)amino)-N-(various substitutions)benzenesulfonamide
Indian Journal of Chemistry, Section B Pub Date : 2020-06-22
Hiren H Variya, Vikram Panchal, G R Patel

In this study all the new synthesized compounds of sulfonamide bearing 4-((2-(5-bromo-1H-pyrazolo[3,4-b]pyridin-1-yl)-2-oxoethyl)amino)-N-(various-substitutions)benzenesul-fonamide have been synthesized by using 1-(5-bromo-1H-pyarazolo[3,4-b]pyridin-1yl)-2-chloroethanone which has been fused with various sulfa drugs in presence of potassium carbonate and DMF. All the derivatives have been recognized by physical properties like melting point and characterization by elemental analysis (CHNS) and various spectral techniques such as FT-IR, 1H and 13C NMR, and ESI-MS. The series of these pyrazolo[3,4-b]pyridin bearing sulfonamide have been synthesized and the final derivatives have been evaluated for bioactivity such as anti-bacterial activity against gram +ve and gram −ve and also screened for their in vitro anti tubercular activity against Mycobacterium tuberculosis H37RV. The results for the synthesized compounds have been compared against standard drugs.

中文翻译:

带有4-(((2-(5-溴-1H-吡唑并[3,4-b]吡啶-1-基)-2-氧代乙基)氨基)-N-的磺酰胺的合成,抗结核和抗菌活性(各种取代基)苯磺酰胺

在这项研究中,所有带有4-((2-(5-bromo-1 H -pyrazolo [3,4- b ] pyridin-1-yl)-2-oxoethyl)amino)-N-(通过使用1-(5-溴-1 H-吡唑并[3,4- b ]吡啶-1基)-2-氯酮合成了各种取代基的苯磺酰胺,在钾的存在下将其与各种磺胺药物融合碳酸盐和DMF。所有衍生物均已通过诸如熔点的物理性质和通过元素分析(CHNS)表征以及各种光谱技术(例如FT-IR,1 H和13 C NMR和ESI-MS )识别。这些吡唑并[3,4- b已经合成了带有]吡啶基的磺酰胺,并且已经评估了最终的衍生物的生物活性,例如针对革兰氏+ ve和革兰氏–ve的抗菌活性,并且还筛选了它们的针对结核分枝杆菌H 37 RV的体外抗结核活性。已将合成化合物的结果与标准药物进行了比较。
更新日期:2020-07-28
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