Bonvicini Francesca, Menegaldo Lisa, Orioli Rebecca, Belluti Federica, Gentilomi Giovanna Angela, Gobbi Silvia, Bisi Alessandra
Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Massarenti 9, 40138 Bologna, Italy.
Department of Chemistry "G. Ciamician", Alma Mater Studiorum-University of Bologna, Via Gobetti 85, 40129 Bologna, Italy.
Molecules. 2025 Jul 15;30(14):2973. doi: 10.3390/molecules30142973.
Fungal infections are recognized as a global health issue, in particular considering the spread of different forms of resistance to the commonly used antifungal drugs and their involvement in the occurrence of co-infections in hospitalized and immunocompromised patients. In this paper, a small series of hybrid compounds were designed and synthesized by linking the privileged chromone and xanthone scaffolds, endowed with recognized antimicrobial potential, to the tert-butylbenzylamino portion of the antifungal drug butenafine, through selected linkers. The results showed for the xanthone-based compound a promising activity towards , , and , for which a high degree of resistance is commonly observed, together with a significant antibacterial potency towards Gram-positive bacteria, such as . Considering that compound displayed favorable selectivity and therapeutic indexes (9.1 and >16, respectively), it appeared as a valuable prototype, deserving further hit-to-lead optimization.
真菌感染被视为一个全球健康问题，尤其是考虑到对常用抗真菌药物的不同形式耐药性的传播，以及它们在住院患者和免疫功能低下患者合并感染发生中的作用。在本文中，通过选定的连接基，将具有公认抗菌潜力的特权色酮和呫吨酮支架与抗真菌药物布替萘芬的叔丁基苄氨基部分相连，设计并合成了一小系列杂化化合物。结果表明，基于呫吨酮的化合物对通常观察到高度耐药性的白色念珠菌、热带念珠菌和近平滑念珠菌具有有前景的活性，同时对革兰氏阳性菌如金黄色葡萄球菌具有显著的抗菌效力。鉴于化合物显示出良好的选择性和治疗指数（分别为9.1和>16），它似乎是一个有价值的原型，值得进一步进行从苗头化合物到先导化合物的优化。
