Synthesis, Stability Studies, and Antifungal Evaluation of Substituted α- and β-2,3-Dihydrofuranaphthoquinones against Sporothrix brasiliensis and Sporothrix schenckii
作者:Patricia Garcia Ferreira、Luana Pereira Borba-Santos、Leticia Noronha、Caroline Deckman Nicoletti、Marcella de Sá Haddad Queiroz、Fernando de Carvalho da Silva、Sônia Rozental、Débora Omena Futuro、Vitor Francisco Ferreira
DOI:10.3390/molecules24050930
日期:——
standard antifungal itraconazole has been recommended as a first-line therapy. However, failure cases in human and feline treatment have been reported in recent years. This study aimed to synthesize several α- and β-2,3-dihydrofuranaphthoquinones and evaluate them against Sporothrix schenckii and Sporothrix brasiliensis-the main etiological agents of sporotrichosis in Brazil. The stability of these compounds
孢子丝菌病是由孢子丝菌(Sporothrix spp。)引起的被忽略的真菌感染,其在世界范围内分布。标准抗真菌伊曲康唑已被推荐作为一线治疗药物。然而,近年来已经报道了人类和猫治疗失败的案例。这项研究旨在合成几种α-和β-2,3-二氢呋喃萘醌,并评估它们对巴西孢子虫病的主要病原体-申氏孢子虫和巴西孢子菌的抵抗力。还研究了这些化合物在不同储存条件下3个月的稳定性。在0、60和90天取出样品并通过1 H-NMR评估,并测试其体外抗真菌药敏性。此外,我们使用扫描电子显微镜评估了最有效和稳定的化合物引起的表面变化,并确定了与伊曲康唑合用时的效果。九种二氢呋喃萘醌具有良好的抗真菌活性和稳定性,MIC值为2⁻32µM。对于这两种物种,化合物6和10是体外活性最高的二氢呋喃萘醌。在真菌中,这些化合物诱导了酵母菌丝的转化以及菌丝和分生孢子结构的改变。化合物10还显示出与伊曲康唑对申氏链球菌的协同活性,ΣFIC指数值为0