Estimation of the lipophilicity of anti-HIV nucleoside analogues by determination of the partition coefficient and retention time on a Lichrospher 60 RP-8 HPLC column.
Estimation of the lipophilicity of anti-HIV nucleoside analogues by determination of the partition coefficient and retention time on a Lichrospher 60 RP-8 HPLC column.
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通过测定 Lichrospher 60 RP-8 HPLC 柱上的分配系数和保留时间来估计抗 HIV 核苷类似物的亲脂性。
DOI：
10.1016/s0006-291x(89)80063-4
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发表时间：
1989
影响因子：
3.1
通讯作者：
E. De Clercq
中科院分区：
文献类型：
--
作者：
J. Balzarini;M. Cools;E. De Clercq
2‘-脱氧核糖苷(DR)、2’，3‘-二氢-2’，3‘-二脱氧核苷(DDR)、2’，3‘-二脱氧核苷(DDR)、3’-氟-2‘，3’-二脱氧核苷(FDDR)和尿嘧啶、胞嘧啶、胸腺嘧啶、鸟嘌呤、腺嘌呤和2，6-二嘌呤的3‘-叠氮-2’，3‘-二脱氧核苷(AZDDR)在Lichrospher 60 RP-8柱上的对数分配系数(PA)与保留时间(RT)呈良好的线性关系(相关系数r&gT=0.970)。在每类化合物中，注意到以下亲脂性递增的顺序：DR<；Dder<；DDR<；FddR<；AzddR。碱基和糖基修饰的嘌呤和嘧啶2‘，3’-双脱氧核苷的亲脂性与结构呈直线关系。
There is a close linear correlation between the log partition coefficient (Pa) of a series of 2′-deoxyriboside (dR), 2′,3′-didehydro-2′,3′-dideoxyriboside (ddeR), 2′,3′-dideoxyriboside (ddR), 3′-fluoro-2′,3′-dideoxyriboside (FddR) and 3′-azido-2′,3′-dideoxyriboside (AzddR) derivatives of uracil, cytosine, thymine, guanine, adenine and 2,6-diaminopurine and their retention times (Rt) on a Lichrospher 60 RP-8 HPLC column (correlation coefficient r > 0.970). Within each class of compounds the following order of increasing lipophilicity was noted : dR < ddeR < ddR < FddR < AzddR. A straight-forward structure-lipophilicity relationship for both base and sugar modified purine and pyrimidine 2′,3′-dideoxynucleosides could be delineated.
影响因子：
5.8
作者：
T. Lin;R. Schinazi;W. Prusoff
通讯作者：
T. Lin;R. Schinazi;W. Prusoff
2,3-dideoxycytidin-2-ene (2,3-dideoxy-2,3-didehydrocytidine) 对人类免疫缺陷病毒的体外抗病毒活性。
影响因子：
5.8
作者：
Lin,TS;Schinazi,RF;Chen,MS;Kinney-Thomas,E;Prusoff,WH
通讯作者：
Prusoff,WH