6-DEOXYCARBOVIR - A XANTHINE-OXIDASE ACTIVATED PRODRUG OF CARBOVIR

被引：10

作者：

VINCE, R

BROWNELL, J

BEERS, SA

机构：

[1] Department of Medicinal Chemistry College of Pharmacy, S.E. University of Minnesota, Minneapolis, MN 55455-0343

来源：

NUCLEOSIDES & NUCLEOTIDES | 1995年 / 14卷 / 1-2期

关键词：

D O I：

10.1080/15257779508014651

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

(-)-(cis)-4-(2-Amino-9H-purin-9-yl)-2-cyclopentenyl carbinol (6-deoxycarbovir) was prepared in order to evaluate prodrug approaches to increased bioavailability of the anti-HN agent, (-)-carbovir. Incubation experiments demonstrated that 6-deoxycarbovir was rapidly converted to (-)-carbovir by the enzyme, xanthine oxidase. Since xanthine oxidase activity is present in both the intestine and liver, a high first pass conversion to carbovir would be expected in vivo.

引用

页码：39 / 44

页数：6

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