ABSTRACT In 1986 a remarkably unusual nucleoside, oxetanocin A (OXT-A) was isolated from the fermentation broth of Bacillus megaterium, and the structural investigation and X-ray crystallographic analysis revealed that OXT-A was the first natural nucleoside having an oxetane ring as a sugar moiety. More interestingly, OXT-A exhibited potent antiviral activity against HSV-1, HSV-2, HCMV, and HIV-1. In this review we will give an overview of the synthetic efforts of OXT-A from the first synthesis in 1987 and the related unusual nucleosides with four-membered heterocyclic sugars as potential antiviral agents, including our works in this area.
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