Synthesis of Novel Cyclopropyl Nucleoside Derivatives as Potential Antiherpetic Agent

새로운 사이클로프로필 뉴크레오사이드 유도체의 합성과 생리활성

  • Kang, Jin-Ah (College of Pharmacy, Laboratory of Medicinal Chemistry, Pusan National University) ;
  • Chun, Pu-Soon (College of Pharmacy, Inje University) ;
  • Moon, Hyung-Ryong (College of Pharmacy, Laboratory of Medicinal Chemistry, Pusan National University)
  • Received : 2012.07.16
  • Accepted : 2012.08.09
  • Published : 2012.08.31

Abstract

Synthesis of novel cyclopropyl pyrimidine and purine nucleoside derivatives 2~8 with ${\alpha}$-configuration was successfully accomplished using an epoxide-ring opening reaction, lactonization, a hydroboration-oxidation reaction and a Mitsunobu reaction as the key steps. Antiviral activities against HSV-1 and -2, HIV-1 and -2, coxsackie B1and B3 viruses and poliovirus were assayed. Three compounds 4, 7 and 8 exhibit cytotoxicity-derived antiviral activity only in HIV-1 and -2.

Keywords

References

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