N6-substituted D-4′-thioadenosine-5′-methyluronamides:: Potent and selective agonists at the human A3 adenosine receptor

被引：84

作者：

Jeong, LS ^{[1
]}

Jin, DZ

Kim, HO

Shin, DH

Moon, HR

Gunaga, P

Chun, MW

Kim, YC

Melman, N

Gao, ZG

Jacobson, KA

机构：

[1] Ewha Womans Univ, Coll Pharm, Med Chem Lab, Seoul 120750, South Korea

[2] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea

[3] Kwangju Inst Sci & Technol, Dept Life Sci, Gwangju 500712, South Korea

[4] NIDDKD, Mol Recognit Sect, Bioorgan Chem Lab, NIH, Bethesda, MD 20892 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 18期

关键词：

D O I：

10.1021/jm034098e

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4'-Thio analogues 3-5 of Cl-IB-MECA (2) (K-i = 1.0 +/- 0.2 nM at the human A(3) adenosine receptor) were synthesized from D-gulono-gamma-lactone via 4-thioribosyl acetate 14 as the key intermediate. All synthesized 4-thionucleosides exhibited higher binding affinity to the human A(3) adenosine receptor than Cl-IB-MECA, among which 4 showed the most potent binding affinity (K-i = 0.28 +/- 0.09 nM). 4 was also selective for A(3) vs human A(1) and human A(2A) receptors by 4800- and 36000-fold, respectively.

引用

页码：3775 / 3777

页数：3

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