Managing primary amoebic meningoencephalitis, induced by Naegleria fowleri poses a complex medical challenge. There is currently no specific anti-amoebic drug that has proven effectiveness against N. fowleri infection. Ongoing research endeavours are dedicated to uncovering innovative treatment strategies, including the utilization of drugs and immune modulators targeting Naegleria infection. In this study, we explored the potential of imidazo[2,1-b]thiazole and imidazooxazole derivatives that incorporate sulfonate and sulfamate groups as agents with anti-amoebic properties against N. fowleri. We assessed several synthesized compounds (1f, 1m, 1q, 1s, and 1t) for their efficacy in eliminating amoebae, their impact on cytotoxicity, and their influence on the damage caused to human cerebral microvascular endothelial (HBEC-5i) cells when exposed to the N. fowleri (ATCC 30174) strain. The outcomes revealed that, among the five compounds under examination, 1m, 1q, and 1t demonstrated notable anti-parasitic effects against N. fowleri (P ≤ 0.05). Compound 1t exhibited the highest anti-parasitic activity, reducing N. fowleri population by 80%. Additionally, three compounds, 1m, 1q, and 1t, significantly mitigated the damage inflicted on host cells by N. fowleri. However, the results of cytotoxicity analysis indicated that while 1m and 1q had minimal cytotoxic effects on endothelial cells, compound 1t caused moderate cytotoxicity (34%). Consequently, we conclude that imidazo[2,1-b]thiazole and imidazooxazole derivatives containing sulfonate and sulfamate groups exhibit a marked capacity to eliminate amoebae viability while causing limited toxicity to human cells. In aggregate, these findings hold promise that could potentially evolve into novel therapeutic options for treating N. fowleri infection.

治疗由福氏耐格里阿米巴引起的原发性阿米巴脑膜脑炎提出了复杂的医学挑战。目前还没有特定的抗阿米巴药物被证明对福氏奈瑟菌感染有效。正在进行的研究致力于发现创新的治疗策略，包括利用针对耐格里虫感染的药物和免疫调节剂。在这项研究中，我们探索了咪唑并[2,1-b]噻唑和咪唑恶唑衍生物的潜力，这些衍生物包含磺酸盐和氨基磺酸盐基团，作为具有抗阿米巴特性的抗阿米巴药物。我们评估了几种合成化合物（1f、1m、1q、1s 和 1t）消除阿米巴原虫的功效、它们对细胞毒性的影响，以及它们对人脑微血管内皮 (HBEC-5i) 细胞暴露于环境中时造成的损伤的影响。福氏奈瑟菌 (ATCC 30174) 菌株。结果显示，在所检测的 5 种化合物中，1m、1q 和 1t 对福氏奈瑟菌具有显着的抗寄生虫作用（P ≤ 0.05）。化合物 1t 表现出最高的抗寄生虫活性，使福氏奈瑟菌数量减少 80%。此外，三种化合物 1m、1q 和 1t 显着减轻了福氏奈瑟菌对宿主细胞造成的损害。然而，细胞毒性分析结果表明，虽然1m和1q对内皮细胞具有最小的细胞毒性作用，但化合物1t引起中等的细胞毒性(34%)。因此，我们得出结论，含有磺酸盐和氨基磺酸盐基团的咪唑并[2,1-b]噻唑和咪唑并恶唑衍生物表现出显着的消除阿米巴原虫活力的能力，同时对人体细胞造成有限的毒性。总的来说，这些发现有望发展成为治疗 N. 福氏菌感染。