Unidad Académica de Ciencias Químicas, Universidad Autónoma de Zacatecas, 98160, Zacatecas, Zac. México.
Facultad de Ciencias Químicas, Universidad Autónoma de San Luis Potosí, 78210, San Luis Potosí, SLP, México.
Mini Rev Med Chem. 2022;22(9):1268-1280. doi: 10.2174/1389557522666220104150051.
The therapeutic potential of the benzimidazole nucleus has been recognized since 1944, and it is an important heterocycle system due to its presence in a wide range of bioactive compounds such as antiviral, anticancer, antibacterial, and so on, where optimization of substituents in this class of pharmacophore has resulted in many drugs. Its broad biological activity stems from physicochemical properties such as hydrogen bond donor-acceptor capability, π→π stacking interactions, coordination bonds with metals as ligands and hydrophobic interactions; properties that allow them to easily bind with a series of biomolecules, including enzymes and nucleic acids, causing a growing interest in these types of molecules. This review aims to present an overview to leading benzimidazole derivatives, as well as to show the importance of the nature and type of substituents at the N1, C2, and C5(6) positions when they are biologically evaluated, which can lead to obtaining potent drug candidate with a significant range of biological activities.
自 1944 年以来，苯并咪唑核的治疗潜力已得到认可，由于其存在于广泛的生物活性化合物中，如抗病毒、抗癌、抗菌等，因此它是一个重要的杂环系统。在这类药效团中优化取代基已导致许多药物的产生。它广泛的生物活性源于物理化学性质，如氢键供体-受体能力、π→π 堆积相互作用、作为配体与金属的配位键以及疏水性相互作用；这些性质使它们能够与一系列生物分子（包括酶和核酸）轻易结合，从而引起人们对这些类型分子的日益关注。本文综述旨在概述主要的苯并咪唑衍生物，并展示在进行生物评价时 N1、C2 和 C5（6）位取代基的性质和类型的重要性，这可能导致获得具有广泛生物活性的有效候选药物。
