Sifaoui Ines, Rodríguez-Expósito Rubén L, Reyes-Batlle María, Rizo-Liendo Aitor, Piñero José E, Bazzocchi Isabel L, Lorenzo-Morales Jacob, Jiménez Ignacio A
Instituto Universitario de Enfermedades Tropicalesy Salud Pública de Canarias, Universidad de La Laguna, Avda Francisco Sanchez s/n, Campus de Anchieta, 38271 La Laguna Tenerife, Islas Canarias, Espana.
Laboratoire Matériaux-Molécules et Applications, University of Carthage, La Marsa Tunisia, Tunisia.
Pathogens. 2019 Aug 23;8(3):130. doi: 10.3390/pathogens8030130.
The current chemotherapy of keratitis relies on few drugs with low potential and limited efficacy, for all this there is an urgent need to identify new classes of anti- agents. In this regard, natural products play an important role in overcoming the current need and medicinal chemistry of natural products represents an attractive approach for the discovery and development of new agents. Ursolic acid, a natural pentacyclic triterpenoid compound, possesses a broad spectrum of activities including anti-. Herein, we report on the development by chemical transformation of an ursolic acid-based series of seven compounds (2-8), one of them reported for the first time. The structure-activity relationship (SAR) analysis of their anti- activity revealed that acylation/ether formation or oxidation enhances their biological profile, suggesting that the hydrophobic moiety contributes to activity, presumably by increasing the affinity and/or cell membrane permeability. These ursolic acid derivatives highlight the potential of this source as a good base for the development of novel therapeutic agents against infections.
目前角膜炎的化疗依赖于少数几种潜力有限且疗效不佳的药物，因此迫切需要鉴定新型抗病原体药物。在这方面，天然产物在满足当前需求方面发挥着重要作用，天然产物药物化学是发现和开发新型药物的一种有吸引力的方法。熊果酸是一种天然五环三萜类化合物，具有广泛的活性，包括抗……。在此，我们报告了通过化学转化开发的一系列七种基于熊果酸的化合物（2-8），其中一种是首次报道。对其抗……活性的构效关系（SAR）分析表明，酰化/醚形成或氧化可增强其生物学特性，这表明疏水部分可能通过增加亲和力和/或细胞膜通透性来促进活性。这些熊果酸衍生物凸显了该来源作为开发新型抗感染治疗药物良好基础的潜力。
