Abstract

The synthesis of 5-acetyl-6-methyl-4-(1,3-diphenyl-1H-pyrazol-4-yl)-3,4-dihydropyrmidin-2(1H)-thione was achieved by one-pot three-component synthesis using CaCl₂ in refluxing EtOH. The starting compound was utilized to synthesize a new series of 5-pyrazolyl; isoxazolyl; pyrimidinyl derivatives via the synthesized chalcone. Also, fused isoxazolo [5,4-d]pyrimidine and pyrazolo[3,4-d]pyrimidine were obtained by the treatment of 5-acetyl derivative with hydroxyl amine and/ or hydrazine hydrate. Also, the thiosemicarbazide derivative was prepared and utilized to synthesize other new thiazole derivatives. The structures of all compounds have been established on the basis of their analytical and spectral data. All compounds was also evaluated for their antibacterial and antifungal activity against various strains of bacteria and fungi. Also, the anti-inflammatory activity of some of synthesized compounds was evaluated using the carrageenan induced paw oedema test in rats using indomethacin as the reference drug.

中文翻译：

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一种高效的5-乙酰基-6-甲基-4-（1,3-二苯基-1 H-吡唑-4-基）-3,4-二氢嘧啶-2（1 H）-亚硫醚作为潜在的抗菌药物和其反应消炎药

摘要

一锅三锅合成了5-乙酰基-6-甲基-4-（1,3-二苯基-1 H-吡唑-4-基）-3,4-二氢嘧啶-2（1 H）-硫酮在回流的EtOH中使用CaCl ₂合成α-组分。该起始化合物被用来合成新的5-吡唑基系列。异恶唑基 嘧啶基衍生物经合成的查尔酮。另外，稠合的异恶唑[5,4- d ]嘧啶和吡唑并[3,4- d通过用羟胺和/或水合肼处理5-乙酰基衍生物获得]嘧啶。同样，制备了硫代氨基脲衍生物，并用于合成其他新的噻唑衍生物。所有化合物的结构都是根据其分析和光谱数据确定的。还评估了所有化合物对各种细菌和真菌菌株的抗菌和抗真菌活性。另外，使用吲哚美辛作为参比药物，采用角叉菜胶诱发的大鼠爪水肿试验评价了某些合成化合物的抗炎活性。