首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis and biological evaluation of novel 6, 7-dimethoxy-3-(4-pyridyl)-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-yl-4-substituted phenylmethanone/ethanone derivatives
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Synthesis and biological evaluation of novel 6, 7-dimethoxy-3-(4-pyridyl)-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-yl-4-substituted phenylmethanone/ethanone derivatives

机译:新型6,7-二甲氧基-3-(4-吡啶基)-2,3,3a,4-四氢茚并[1,2-c]吡唑-2-基-4-取代的苯甲酮/乙酮衍生物的合成及生物评价

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A series of 6,7-dimethoxy-3-(4-pyridyl)-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-yl-4-substituted phenylmethanone/ethanone derivatives were synthesized and in vitro activity against mycobacterium tuberculosis (MTB) and INHR-MTB were carried out. Among the synthesized compounds, compound (4h) 6,7-dimethoxy-3-(4-pyridyl)-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-yl-4-pyridyl methanone was found to be the most active agent against MTB and INHR-MTB with a minimum inhibitory concentration of 0.22 μM.
机译:合成了一系列6,7-二甲氧基-3-(4-吡啶基)-2,3,3a,4-四氢茚并[1,2-c]吡唑-2-基-4-取代的苯甲酮/乙酮衍生物,并在进行了针对结核分枝杆菌(MTB)和INHR-MTB的体外活性。在合成的化合物中,化合物(4h)为6,7-二甲氧基-3-(4-吡啶基)-2,3,3a,4-四氢茚并[1,2-c]吡唑-2-基-4-吡啶基甲酮。被发现是对MTB和INHR-MTB最具活性的药物,最低抑制浓度为0.22μM。

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