Acanthamoeba is a genus of free-living amoebae, pervasively found in the environment. Most of its pathogenic species are the causative agent of sight-threatening Acanthamoeba keratitis and fatal granulomatous amoebic encephalitis. Despite the advancements in the field of chemotherapy, treating Acanthamoeba infections is still challenging due to incomplete knowledge of the complicated pathophysiology. In case of infection, the treatment regimen for the patients is often ineffective due to delayed diagnosis, poor specificity, and side-effects. Besides the resistance of Acanthamoeba cysts to most of the drugs, the recurrence of infection further complicates the recovery. Thus, it is necessary to develop an effective treatment which can eradicate these rare, but serious infections. Based on various computational and in vitro studies, it has been established that the synthetic scaffolds such as heterocyclic compounds may act as potential drug leads for the development of antiamoebic drugs. In this review, we report different classes of synthetic compounds especially heterocyclic compounds which have shown promising results against Acanthamoeba. Moreover, the antiamoebic activities of synthetic compounds with their possible mode of actions against Acanthamoeba, have been summarized and discussed in this review.

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药物化学在发现抗棘阿米巴感染药物中的应用

棘阿米巴是一种自由生活的变形虫，普遍存在于环境中。其大部分致病菌是威胁视力的棘阿米巴角膜炎和致命的肉芽肿性阿米巴脑炎的病原体。尽管化疗领域取得了进步，但由于对复杂的病理生理学知识不完整，治疗棘阿米巴感染仍然具有挑战性。在感染的情况下，由于延误诊断、特异性差和副作用，对患者的治疗方案往往无效。除了对棘阿米巴的抵抗力囊肿对大多数药物来说，感染的复发使恢复更加复杂。因此，有必要开发一种可以根除这些罕见但严重的感染的有效治疗方法。基于各种计算和体外研究，已确定合成支架（如杂环化合物）可作为开发抗阿米巴药物的潜在药物先导物。在这篇综述中，我们报告了不同类别的合成化合物，尤其是杂环化合物，它们已显示出对抗棘阿米巴的有希望的结果。此外，本综述总结和讨论了合成化合物的抗阿米巴活性及其对棘阿米巴的可能作用方式。