Synthesis of 5'-3H-2-Amino-6-cyclopropylaminopurine Nucleosides

作     者：YANG Zhen-Jun Chung K. Chu ZHANG Li-He 

作者机构：School of Pharmaceutical Sciences Peking University Health Science Center Beijing 100083 College of Pharmacy The University of Georgia Athens Georgia 30602 College of Pharmacy The University of Georgia Athens Georgia 30602 

出 版 物：《有机化学》 (Chinese Journal of Organic Chemistry)

年 卷 期：2003年第23卷第Z1期

页      面：35-36页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

主　　题：oral administration in vitro 

摘      要： We have described a novel use of the D4G prodrug (Cyclo-D4G) approach to stabilize the nucleoside and maintain the anti-HIV activity. β-D-Dioxolanyl-2-amino-6-cyclopropylaminopurine (10, DACP) was synthesized as a prodrug of β-D-dioxolanyl guanine (DXG) and showed potent anti-HIV activity in vitro (EC50=0.18 μmol·L-1 The pharmacokinetics of Cyclo-D4G and DACP following intravenous and oral administration of DACP to rhesusmonkeys and rats did not give D4G and DXG as detectable metabolic products by HPLC. Therefore the radio labeled Cyclo-D4G and DACP are necessary for the pharmacokinetics studies in detail.……