Preparatory Year Deanship. Basic Science Department, Prince Sattam Bin Abdulaziz University, 151, Alkharj, 11942, KSA, Saudi Arabia.
ChemistryOpen. 2024 Jun;13(6):e202400070. doi: 10.1002/open.202400070. Epub 2024 Apr 29.
This study reports the design, synthesis, and antibacterial evaluation of a library of novel polyheterocyclic derivatives featuring a unique fused pyrimidopyridopyrazole moiety. A cyclocondensation reaction between an amino-pyrazolopyridopyrimidine precursor and malonates afforded a series of pyrimidopyridopyrazolopyrimidine derivatives. Further diversification was achieved through nucleophilic cyclocondensation, yielding a collection of complex polyheterocyclic systems encompassing various ring structures. All synthesized compounds were rigorously characterized using spectroscopic techniques and elemental analysis. The antibacterial activity of the newly synthesized compounds was assessed against a panel of Gram-positive and Gram-negative bacteria. Notably, several compounds exhibited promising antibacterial activity, highlighting their potential as leads for the development of novel antibiotics.
本研究报告了一类新型多杂环衍生物的设计、合成和抗菌评价,这些衍生物具有独特的融合嘧啶并吡啶并吡唑部分。通过氨基-吡唑并吡啶并嘧啶前体与丙二酸酯之间的环缩合反应,得到了一系列嘧啶并吡啶并吡唑嘧啶衍生物。进一步通过亲核环缩合反应实现了多样化,得到了一系列复杂的多杂环体系,包含各种环结构。所有合成的化合物都经过了严格的光谱技术和元素分析表征。新合成的化合物的抗菌活性通过对一组革兰氏阳性和革兰氏阴性细菌进行评估。值得注意的是,一些化合物表现出了有前景的抗菌活性,凸显了它们作为开发新型抗生素的潜在先导化合物的潜力。