Unidad Académica Multidisciplinaria Reynosa-Rodhe, Universidad Autónoma de Tamaulipas, Reynosa 88779, México.
Laboratorio de Biotecnología Farmacéutica, Centro de Biotecnología Genómica, Instituto Politécnico Nacional, Boulevard del Maestro, s/n, Esq. Elías Piña, Reynosa 88710, México.
Molecules. 2024 Sep 30;29(19):4652. doi: 10.3390/molecules29194652.
Mycetoma is currently considered as a neglected tropical disease. The incidence of mycetoma is unknown but most of the worldwide cases are present in the "mycetoma belt" including countries like Mexico, India, Senegal, and others. The treatment of mycetoma depends on the etiological agent responsible for the case. Treatment success reaches 60 to 90%; however, common treatment has been reported to be ineffective in some cases, due in part to resistance to the prescribed antibiotics. Therefore, it is necessary to develop new therapeutic options. In the past two decades, quinoxaline derivatives have shown relevance as antibacterial agents. Therefore, in this work, esters of quinoxaline 1,4-di--oxide derivatives were evaluated in vitro against the reference strain CECT-3052 from , six clinical isolates, and macrophages J774A.1 to determine their cytotoxicity and security index. Additionally, nine reference drugs were evaluated as controls. The results show that nine esters of quinoxaline 1,4-di--oxide derivatives had a minimum inhibitory concentration (MIC) < 1 µg/mL against the reference strain and four of them (, , , and ) had an MIC < 1 µg/mL against the clinical isolates. Therefore, the scaffold quinoxaline 1,4-di--oxide could be used to develop new and more potent antinocardial agents.
足菌肿目前被认为是一种被忽视的热带病。足菌肿的发病率尚不清楚，但世界上大多数病例都出现在“足菌肿带”，包括墨西哥、印度、塞内加尔等国家。足菌肿的治疗取决于导致该病的病原体。治疗成功率达到 60%至 90%；然而，据报道，常规治疗在某些情况下无效，部分原因是对规定抗生素的耐药性。因此，有必要开发新的治疗方案。在过去的二十年中，喹喔啉衍生物已被证明是具有抗菌活性的药物。因此，在这项工作中，评估了喹喔啉 1,4-二氧化物衍生物的酯类化合物在体外对参考菌株 CECT-3052（来自 ）、六个临床分离株和巨噬细胞 J774A.1 的活性，以确定其细胞毒性和安全指数。此外，还评估了九种参考药物作为对照。结果表明，九种喹喔啉 1,4-二氧化物衍生物的酯类化合物对参考菌株的最小抑菌浓度（MIC）<1µg/mL，其中四种（ 、 、 、 ）对临床分离株的 MIC<1µg/mL。因此，喹喔啉 1,4-二氧化物支架可用于开发新型、更有效的抗心肌药物。
