Boddapati S N Murthy, Chalapaka Bhuvaneswari, Kola Abraham Emmanuel, Jonnalagadda Sreekantha Babu
School of Chemistry & Physics, College of Agriculture, Engineering & Science, University of KwaZulu-Natal, Westville Campus, P Bag X 54001, Durban, 4000, South Africa.
Department of Chemistry, Sir C R Reddy College, P G Courses, Eluru, A.P., 534007, India.
Top Curr Chem (Cham). 2025 Jul 1;383(3):26. doi: 10.1007/s41061-025-00509-9.
Research on heterocyclic compounds is an area of continuous focus, capturing the interest of both synthetic and natural product chemists. Indazoles are one of the rare heterocycles that are available in nature. Indazole and its derivatives are one of the most important classes of heterocycles in pharmacological molecules. The structurally different indazole motifs, with impressive bioactivity, have drawn increasing attention from medicinal chemists in recent years for the continuous development of novel drug moieties. Thus, knowledge of the biological activities and synthetic pathways of indazole scaffolds is essential to enhancing further developments in the number of indazole-based lead molecules. The goal of the present review is to highlight information on the biological properties of some existing indazole-based drugs and activities of novel bioactive indazole compounds in clinical trails, with specific attention to the most recent advances in various synthetic strategies towards indazole and its derivatives over the past 7 years (2017-2024). Moreover, we discuss the substrate tolerance and mechanistic insights for most of the summarized synthetic protocols.
杂环化合物的研究是一个持续受到关注的领域，吸引了合成化学家和天然产物化学家的兴趣。吲唑是自然界中罕见的杂环之一。吲唑及其衍生物是药理分子中最重要的杂环类之一。结构不同的吲唑基序具有令人印象深刻的生物活性，近年来因其作为新型药物部分的不断发展而受到药物化学家越来越多的关注。因此，了解吲唑支架的生物活性和合成途径对于增加基于吲唑的先导分子数量的进一步发展至关重要。本综述的目的是强调一些现有基于吲唑的药物的生物学特性以及新型生物活性吲唑化合物在临床试验中的活性信息，特别关注过去七年（2017 - 2024年）中针对吲唑及其衍生物的各种合成策略的最新进展。此外，我们还讨论了大多数总结的合成方案的底物耐受性和机理见解。
