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近期发现的具有前景的香芹酚药理学支架:综述。

The recent discovery of a promising pharmacological scaffold derived from carvacrol: A review.

机构信息

Department of Chemical Sciences, Faculty of Science and Technology, Universiti Kebangsaan Malaysia, 43600 UKM Bangi, Selangor, Malaysia; International Joint Department of Materials Science and Engineering Between National University of Malaysia and Gifu University, Graduate School of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan; Department of Chemistry, Universitas Negeri Malang, Jl. Semarang No. 5 Malang, Indonesia.

Department of Chemical Sciences, Faculty of Science and Technology, Universiti Kebangsaan Malaysia, 43600 UKM Bangi, Selangor, Malaysia.

出版信息

Bioorg Med Chem Lett. 2024 Sep 1;109:129826. doi: 10.1016/j.bmcl.2024.129826. Epub 2024 Jun 1.

Abstract

Carvacrol, called CA, is a dynamic phytoconstituent characterized by a phenol ring abundantly sourced from various natural reservoirs. This versatile scaffold serves as a pivotal template for the design and synthesis of novel drug molecules, harboring promising biological activities. The active sites positioned at C-4, C-6, and the hydroxyl group (-OH) of CA offer fertile ground for creating potent drug candidates from a pharmacological standpoint. In this comprehensive review, we delve into diverse synthesis pathways and explore the biological activity of CA derivatives. We aim to illuminate the potential of these derivatives in discovering and developing efficacious treatments against a myriad of life-threatening diseases. By scrutinizing the structural modifications and pharmacophore placements that enhance the activity of CA derivatives, we aspire to inspire the innovation of novel therapeutics with heightened potency and effectiveness.

摘要

香芹酚,简称 CA,是一种动态植物成分,其特征是具有丰富来源的酚环,广泛存在于各种天然资源中。这个多功能的支架可以作为设计和合成新型药物分子的关键模板,具有有前途的生物活性。CA 的活性位点位于 C-4、C-6 和羟基 (-OH) 位置,为从药理学角度开发出有效的药物候选物提供了肥沃的土壤。在这篇全面的综述中,我们探讨了不同的合成途径,并研究了 CA 衍生物的生物学活性。我们旨在阐明这些衍生物在发现和开发针对多种危及生命疾病的有效治疗方法方面的潜力。通过仔细研究能够提高 CA 衍生物活性的结构修饰和药效团放置,我们希望能够激发具有更高效力和有效性的新型治疗药物的创新。

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