Kumar Pawan, Bhatia Rohit, Rangra Naresh Kumar
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab, 142001, India.
Chitkara University School of Pharmacy, Chitkara University, Himachal Pradesh, 174103, India.
Mol Divers. 2025 Feb;29(1):783-816. doi: 10.1007/s11030-024-10869-x. Epub 2024 Jul 31.
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.
蠕虫病影响着全球数十亿人，是一个重大的健康问题，在卫生条件差的贫困地区尤为严重。蠕虫复杂的解剖结构需要专门的治疗方法。目前尚无有效的抗蠕虫感染疫苗。抗蠕虫药对于对抗这些感染至关重要，它作用于寄生虫的神经肌肉功能而不伤害宿主。然而，对现有抗蠕虫药，尤其是苯并咪唑类药物产生的耐药性，正成为一个日益严峻的全球挑战。本综述深入探讨了先前合成的核心抗蠕虫支架（苯并咪唑、香豆素、吡唑啉、三唑等）的构效关系，以阐明它们有前景的抗蠕虫活性。了解这些新型苯并咪唑衍生物、香豆素衍生物等的构效关系，对于设计有效的抗蠕虫药、克服耐药性以及优化疗效以应对不断升级的全球蠕虫感染负担至关重要。在本综述中，我们涵盖了最近研究的（从2019年至今）具有有前景抗蠕虫活性的化合物。本综述将对从事抗蠕虫药研究的药理学和药物化学研究人员有用，他们使用各种支架，如氨基苯并噻唑、苯并咪唑、苯并噻唑、香豆素、色烯、螺缩酮、吡唑啉、三唑等，来设计新型强效抗蠕虫化合物。
