期刊
DRUG DEVELOPMENT RESEARCH
卷 77, 期 5, 页码 241-250出版社
WILEY-BLACKWELL
DOI: 10.1002/ddr.21317
关键词
nitroxanthines; adenosine receptors; nitrate esters
资金
- HSCST, Haryana, India
- Association of Commonwealth Universities, United Kingdom
A new series of 1,3-dimethylxanthine derivatives bearing 8-(2-nitroaryl) residue was synthesized and evaluated for affinity for recombinant human adenosine receptors subtypes. Nitrate esters of 7-substituted-1,3-dimethyl-8-phenylxanthines were also synthesized and tested. Introducing a nitro substituent at the 2-position of the 8-substituted phenyl ring resulted in generally low affinity for adenosine receptors (ARs), selectivity toward the A(2A) subtype was enhanced in some of the compounds. 8-(4-Cyclopentyloxy-5-methoxy-2-nitrophenyl)-1,3-dimethylxanthine (9e) proved to be a potent compound among the 2-nitrophenyl substituted xanthines exhibiting a K-i=1 M at human A(2A) ARs with at least 30 fold selectivity versus human A(1) and A(2B) ARs. Replacement of 8-chloropropoxy phenyl with 8-nitrooxypropoxy phenyl resulted in a negligible change in binding affinity of the 8-substituted xanthines for various AR subtypes. Drug Dev Res 77 : 241-250, 2016. (c) 2016 Wiley Periodicals, Inc.
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