Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala - 147002, India.
Mini Rev Med Chem. 2019;19(8):624-646. doi: 10.2174/1389557517666171101104024.
Structural resemblance of benzimidazole nucleus with purine nucleus in nucleotides makes benzimidazole derivatives attractive ligands to interact with biopolymers of a living system. The most prominent benzimidazole compound in nature is N-ribosyldimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. This structural similarity prompted medicinal chemists across the globe to synthesize a variety of benzimidazole derivatives and to screen those for various biological activities, such as anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimicrobial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant and antidiabetic activities. Hence, benzimidazole nucleus is considered as a privileged structure in drug discovery, and it is exploited by many research groups to develop numerous compounds that are purported to be antimicrobial. Despite a large volume of research in this area, no novel benzimidazole derived compound has emerged as clinically effective antimicrobial drug. In the present review, we have compiled various reports on benzimidazole derived antimicrobials, classified as monosubstituted, disubstituted, trisubstituted and tetrasubstituted benzimidazoles, bisbenzimidazoles, fused-benzimidazoles, and benzimidazole derivative-metal complexes. The purpose is to collate these research reports, and to generate a generalised outlay of benzimidazole derived molecules that can assist the medicinal chemists in selecting appropriate combination of substituents around the nucleus for designing potent antimicrobials.
苯并咪唑核与核苷酸中的嘌呤核在结构上具有相似性,这使得苯并咪唑衍生物成为与生物体系中生物聚合物相互作用的有吸引力的配体。自然界中最突出的苯并咪唑化合物是 N-核糖基二甲苯并咪唑,它作为维生素 B12 中钴的轴向配体。这种结构上的相似性促使全球的药物化学家合成了各种苯并咪唑衍生物,并对这些衍生物进行了各种生物活性的筛选,如抗癌、激素拮抗剂、抗病毒、抗 HIV、驱虫、抗原生动物、抗菌、降压、抗炎、镇痛、抗焦虑、抗过敏、凝血、抗凝、抗氧化和抗糖尿病活性。因此,苯并咪唑核被认为是药物发现中的一个特权结构,许多研究小组都利用它来开发据称具有抗菌作用的许多化合物。尽管在这一领域进行了大量的研究,但没有一种新型的苯并咪唑衍生化合物作为临床有效的抗菌药物出现。在本综述中,我们汇编了各种关于苯并咪唑衍生抗菌剂的报告,这些抗菌剂分为单取代、二取代、三取代和四取代苯并咪唑、双苯并咪唑、稠合苯并咪唑和苯并咪唑衍生物-金属配合物。目的是整理这些研究报告,并生成一个概括性的苯并咪唑衍生分子图,以帮助药物化学家选择合适的核周围取代基组合,用于设计有效的抗菌剂。