Bhushan Rashmi Gupta, Vince Robert
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Bioorg Med Chem. 2002 Jul;10(7):2325-33. doi: 10.1016/s0968-0896(02)00063-9.
A series of 2',3'-exo-methylene carbocyclic nucleosides was synthesized as potential antiviral agents. These compounds were built on a bicyclo[3.1.0]hexane template that exhibits a rigid pseudoboat conformation and is capable of maintaining an identical conformation in solid state and in solution. The structures of the synthesized compounds were elucidated by NMR and X-ray crystallography. All the compounds were tested as anti-HIV and anti-HSV agents. The chemically synthesized 5'-triphosphate analogue of 7 was evaluated directly as a reverse transcriptase inhibitor.
合成了一系列2',3'-外向亚甲基碳环核苷作为潜在的抗病毒剂。这些化合物基于双环[3.1.0]己烷模板构建，该模板呈现出刚性假船式构象，并且能够在固态和溶液中保持相同的构象。通过核磁共振（NMR）和X射线晶体学阐明了合成化合物的结构。所有化合物都作为抗HIV和抗HSV剂进行了测试。对化学合成的7的5'-三磷酸类似物直接作为逆转录酶抑制剂进行了评估。
