Herein, the building block synthon 2-cyano-3-(1,3-diphenyl-1H-pyrazol-4-yl)acryloyl chloride 4 was synthesized and utilized for construction of a wide variety of nitrogen heterocycles encompassing a pyrazole scaffold via treatment with some nitrogen nucleophiles. The seven membered heterocycles 14–16 and 20 were constructed from the reaction of the acid chloride 4 with 1,4-binucleophilic reagents such as 2-aminophenol, 2-aminoaniline, 2-aminothiophenol, and thiosemicarbazide, respectively. The structures of all the synthesized heterocycles were elucidated from their elemental and spectral analysis. Antiviral activity screening of products obtained against rotavirus (RV) revealed that compounds 3, 12, 13, 15, and 16 exhibited high reduction effect on RV titer of ≥ 2 log₁₀ TCID₅₀. Thus, these compounds can be possible candidates of anti-RV agents.

中文翻译：

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吡唑支架与部分氮杂环的合成及抗轮状病毒活性

在此，合成了合成基元合成2-氰基-3-（1,3-二苯基-1H-吡唑-4-基）丙烯酰氯4，并通过处理用于构建包括吡唑骨架的多种氮杂环。与一些氮亲核试剂。七元杂环14 - 16和20是从酰氯的反应构建4分别使用1,4-双亲核试剂，例如2-氨基苯酚，2-氨基苯胺，2-氨基硫酚和硫代氨基脲。从其元素和光谱分析中阐明了所有合成杂环的结构。抗病毒活性筛选的抗轮状病毒（RV）获得的产物表明，化合物3，12，13，15，和1 6显示对≥2日志的RV滴度高降低效果₁₀ TCID ₅₀。因此，这些化合物可能是抗RV剂的候选者。