Unsal Tan Oya, Zengin Merve
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Arch Pharm (Weinheim). 2022 Mar;355(3):e2100383. doi: 10.1002/ardp.202100383. Epub 2021 Nov 11.
Acrylonitrile is a fascinating scaffold widely found in many natural products, drugs, and drug candidates with various biological activities. Several drug molecules such as entacapone, rilpivirine, teriflunomide, and so forth, bearing an acrylonitrile moiety have been marketed. In this review, diverse synthetic strategies for constructing desired acrylonitriles are discussed, and the different biological activities and medicinal significance of various acrylonitrile derivatives are critically evaluated. The information gathered is expected to provide rational guidance for the development of clinically useful agents from acrylonitriles.
丙烯腈是一种引人注目的骨架结构,广泛存在于许多具有各种生物活性的天然产物、药物及候选药物中。几种含有丙烯腈部分的药物分子,如恩他卡朋、利匹韦林、特立氟胺等,已上市销售。在本综述中,讨论了构建所需丙烯腈的各种合成策略,并对各种丙烯腈衍生物的不同生物活性和药用意义进行了批判性评估。所收集的信息有望为从丙烯腈开发临床有用药物提供合理指导。