Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A(1) receptor antagonists and their biological evaluation

Koul Summon; Ramdas Vidya; Barawkar Dinesh A.Waman Yogesh B.Prasad NeelaMadadi Santosh KumarShejul Yogesh D.Bonagiri RajeshBasu SujayMenon SurajReddy Srinivasa B.Chaturvedi SandhyaChennamaneni Srinivas RaoBedse GauravThakare RhishikeshGundu JayasagarChaudhary SumitDe SiddharthaMeru Ashwinkumar V.Palle VenkataChugh AnitaMookhtiar Kasim A.

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Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A(1) receptor antagonists and their biological evaluation

机译：Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A(1) receptor antagonists and their biological evaluation

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Multipronged approach was used to synthesize a library of diverse C-8 cyclopentyl hypoxanthine analogs from a common intermediate III. Several potent and selective compounds were identified and evaluated for pharmacokinetic (PK) properties in Wistar rats. One of the compounds 14 with acceptable PK parameters was selected for testing in in vivo primary acute diuresis model. The compound demonstrated significant diuretic activity in this model. (C) 2017 Elsevier Ltd. All rights reserved.

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《Bioorganic and medicinal chemistry》 |2017年第6期|1963-1975|共13页
作者
Koul Summon; Ramdas Vidya; Barawkar Dinesh A.Waman Yogesh B.Prasad NeelaMadadi Santosh KumarShejul Yogesh D.Bonagiri RajeshBasu SujayMenon SurajReddy Srinivasa B.Chaturvedi SandhyaChennamaneni Srinivas RaoBedse GauravThakare RhishikeshGundu JayasagarChaudhary SumitDe SiddharthaMeru Ashwinkumar V.Palle VenkataChugh AnitaMookhtiar Kasim A.;
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Advinus Therapeut Ltd, Drug Discovery Unit, Pune 411057, Maharashtra, India;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Adenosine; Rolofylline; BG-9928; Diuresis; Hypoxanthine; Glomerular;

Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A(1) receptor antagonists and their biological evaluation

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