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Privileged small molecules against neglected tropical diseases: A perspective from structure activity relationships
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2024-04-16 , DOI: 10.1016/j.ejmech.2024.116396
J. Abbasi Shiran , B. Kaboudin , N. Panahi , N. Razzaghi-Asl

Neglected tropical diseases (NTDs) comprise diverse infections with more incidence in tropical/sub-tropical areas. In spite of preventive and therapeutic achievements, NTDs are yet serious threats to the public health. Epidemiological reports of world health organization (WHO) indicate that more than 1.5 billion people are afflicted with at least one NTD type. Among NTDs, leishmaniasis, chagas disease (CD) and human African trypanosomiasis (HAT) result in substantial morbidity and death, particularly within impoverished countries. The statistical facts call for robust efforts to manage the NTDs. Currently, most of the anti-NTD drugs are engaged with drug resistance, lack of efficient vaccines, limited spectrum of pharmacological effect and adverse reactions. To circumvent the issue, numerous scientific efforts have been directed to the synthesis and pharmacological development of chemical compounds as anti-infectious agents. A survey of the anti-NTD agents reveals that the majority of them possess privileged nitrogen, sulfur and oxygen-based heterocyclic structures. In this review, recent achievements in anti-infective small molecules against parasitic NTDs are described, particularly from the SAR (Structure activity relationship) perspective. We also explore current advocating strategies to extend the scope of anti-NTD agents.

中文翻译:

对抗被忽视的热带疾病的特权小分子:结构活性关系的视角

被忽视的热带病 (NTD) 包括多种感染,在热带/亚热带地区发病率较高。尽管在预防和治疗方面取得了一定的成就,但被忽视的热带疾病仍然对公众健康构成严重威胁。世界卫生组织(WHO)的流行病学报告表明,超过15亿人患有至少一种NTD类型。在 NTD 中,利什曼病、恰加斯病 (CD) 和非洲人类锥虫病 (HAT) 导致大量发病和死亡,特别是在贫困国家。统计事实表明需要大力管理被忽视的热带病。目前,大多数抗NTD药物都存在耐药性、缺乏高效疫苗、药理作用谱有限以及不良反应等问题。为了解决这个问题,许多科学努力致力于作为抗感染剂的化合物的合成和药理学开发。对抗 NTD 药物的调查表明,它们中的大多数都具有独特的氮、硫和氧基杂环结构。在这篇综述中,描述了抗寄生性 NTD 的抗感染小分子的最新成就,特别是从 SAR(结构活性关系)的角度。我们还探讨了当前扩大抗 NTD 药物范围的倡导策略。
更新日期:2024-04-16
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