STRUCTURE-BASED DESIGN OF INHIBITORS OF PURINE NUCLEOSIDE PHOSPHORYLASE .2. 9-ALICYCLIC AND 9-HETEROALICYCLIC DERIVATIVES OF 9-DEAZAGUANINE

被引:48
作者
SECRIST, JA
NIWAS, S
ROSE, JD
BABU, YS
BUGG, CE
ERION, MD
GUIDA, WC
EALICK, SE
MONTGOMERY, JA
机构
[1] BIOCRYST PHARMACEUT INC,2190 PKWY LAKE DR,BIRMINGHAM,AL 35244
[2] SO RES INST,BIRMINGHAM,AL 35255
[3] CIBA GEIGY CORP,SUMMIT,NJ 07901
[4] UNIV ALABAMA,BIRMINGHAM,AL 35294
关键词
D O I
10.1021/jm00065a007
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Alicyclic and heteroalicyclic derivatives of 9-deazaguanine (2-amino-1,5-dihydro-4H-pyrrolo[3,2-d][pyrimidin-4-one) d] [pyrimidin-4-one) are, with one exception, potent inhibitors of purine nucleoside phosphorylase (PNP) equaling the corresponding 9-arylmethyl derivatives previously investigated. The mode of binding of these compounds to PNP was determined by X-ray crystallography.
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页码:1847 / 1854
页数:8
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