具有驱虫活性的支架:最新进展和 SAR 研究。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Pawan Kumar, Rohit Bhatia, Naresh Kumar Rangra
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引用次数: 0

摘要

蠕虫病影响着全球数十亿人的健康,尤其是在卫生条件不足的贫困地区,是一个重大的健康问题。螺旋体的解剖结构复杂,需要专门的治疗方法。目前还没有针对蠕虫感染的有效疫苗。抗蠕虫药是防治这些感染的关键,它针对寄生虫的神经肌肉功能而不伤害宿主。然而,现有抗蠕虫药(尤其是苯并咪唑类)的抗药性的出现带来了日益严峻的全球性挑战。本综述深入研究了以前合成的核心抗寄生虫药物支架--苯并咪唑、香豆素、吡唑啉、三唑等的结构-活性关系,以阐明它们具有良好的抗寄生虫活性。了解这些新型苯并咪唑衍生物、香豆素衍生物及其他衍生物的结构-活性关系,对于设计强效驱虫药、克服抗药性和优化药效以应对全球不断增加的蠕虫感染负担至关重要。在本综述中,我们将介绍最近研究的具有良好抗蠕虫活性的化合物(从 2019 年至今)。本综述将有助于药理学和药物化学领域的研究人员利用各种支架(如氨基苯并噻唑、苯并咪唑、苯并噻唑、香豆素、铬烯、螺酮、吡唑啉、三唑等)设计新型强效驱虫化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Scaffolds imparting anthelmintic activity: recent advancements and SAR studies.

Scaffolds imparting anthelmintic activity: recent advancements and SAR studies.

Helminthiasis, affecting billions globally, poses a significant health concern, especially in impoverished regions with inadequate sanitation. The intricate anatomical complexity of helminths requires specialized treatment approaches. There is currently no effective vaccine against helminth infections. Anthelmintics, crucial for combating these infections, target neuromuscular functions in parasites without harming the host. However, the emergence of resistance to existing anthelmintics, notably benzimidazoles, presents a growing global challenge. This review delves into the structure-activity relationship of previously synthesized core anthelmintic scaffolds-Benzimidazole, coumarin, pyrazoline, triazole, and others-to elucidate their promising anthelmintic activities. Understanding the structure-activity relationship of these novel benzimidazole derivatives, Coumarin derivatives, and others is crucial in designing potent anthelmintics, overcoming resistance, and optimizing efficacy to combat the escalating global burden of helminth infections. In the present review, we cover recently studied compounds (from the year 2019 to till date) which have promising anthelmintic activity. This review will be useful for the pharmacology and medicinal chemistry researchers working in the area anthelmintics with various scaffolds like aminobenzothiazole, benzimidazole, benzothiazole, coumarin, chromene, spiroketal, pyrazoline, triazole, etc. to design novel potent anthelmintic compound.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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