SYNTHESIS OF ENANTIOMERICALLY PURE (2'R,5'S)-(-)-1-[2-(HYDROXYMETHYL)OXATHIOLAN-5-YL]CYTOSINE AS A POTENT ANTIVIRAL AGENT AGAINST HEPATITIS-B VIRUS (HBV) AND HUMAN-IMMUNODEFICIENCY-VIRUS (HIV)

被引:173
作者
BEACH, JW
JEONG, LS
ALVES, AJ
POHL, D
KIM, HO
CHANG, CN
DOONG, SL
SCHINAZI, RF
CHENG, YC
CHU, CK
机构
[1] UNIV GEORGIA,COLL PHARM,DEPT MED CHEM,ATHENS,GA 30602
[2] YALE UNIV,SCH MED,DEPT PHARMACOL,NEW HAVEN,CT 06510
[3] EMORY UNIV,VET ADM MED CTR,SCH MED,ATLANTA,GA 30033
关键词
D O I
10.1021/jo00034a006
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of the enantiomerically pure 2'R,5'S-(-) form of BCH-189 from L-gulose has been accomplished, and this isomer has been found to exhibit the most potent anti-HIV and anti-HBV activities among the four possible isomers. This is the first example of an "L-like" nucleoside which is more potent than its "D-like" isomer.
引用
收藏
页码:2217 / 2219
页数:3
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