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Design and Synthesis of Novel 2'(β)-Fluoro-3'(α)-hydroxy-threose Nucleosides: Iso-FMAU Analogues as Potent Antiviral Agents

초록

영어

Novel 2'(β)-fluoro-3'(α)-hydroxy-threose nucleosides (iso-FMAU) as antiviral agents were designed and racemically synthesized from Solketal. Condensation successfully proceeded from a glycosyl donor 9 under Vorbrüggen conditions yielded the nucleoside analogues. Ammonolysis and hydrolysis of isopropylidene protection group gave the desired nucleoside analogues 12, 15, 18, and 19. The antiviral activities of the synthesized compounds were evaluated against the HIV-1, HSV-1, HSV-2 and HCMV. Compound 12 displayed some anti-HCMV activity (EC50=24.7 μg/ml) without exhibiting any cytotoxicity up to 100 μM.

목차

Abstract
 1. Introduction
 2. Experimental Section
 3. Results and Discussion
 4. Conclusion
 References

저자정보

  • Seyeon Kim BK-21 Project Team, College of Pharmacy, Chosun University, Kwangju 501-759, Korea
  • Jun-Pil Jee BK-21 Project Team, College of Pharmacy, Chosun University, Kwangju 501-759, Korea
  • Joon Hee Hong BK-21 Project Team, College of Pharmacy, Chosun University, Kwangju 501-759, Korea

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