‎1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine ‎Derivatives as Highly Potent and Selective Human A(2B) ‎Adenosine Receptor Antagonists | An-Najah Staff

‎1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine ‎Derivatives as Highly Potent and Selective Human A(2B) ‎Adenosine Receptor Antagonists

2384's picture

Tue, 2014-07-01 09:49 — Abdel Naser Zaid

Journal Title, Volume, Page:

Bioorg Med Chem.;16(5):2419-30. Epub 2007 Nov 28.

Year of Publication:

2008

Link:

http://www.sciencedirect.com/science/article/pii/S0968089607010279

Authors:

Abdel Naser Zaid

College of Pharmacy, An-Najah National University, Nablus, Palestine

Current Affiliation:

Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine

[email protected]

Mojgan Aghazadeh Tabrizi

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Pier Giovanni Baraldi

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Delia Preti

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Romeo Romagnoli

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Giulia Saponaro

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Stefania Baraldi

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Allan R. Moorman

King Pharmaceuticals, Inc., Research and Development, 4000 CentreGreen Way, Suite 300, Cary, North Carolina 27513, Italy

Katia Varani

Dipartimento di Medicina Clinica e Sperimentale-Sezione di Farmacologia, Università di Ferrara, 44100 Ferrara, Italy

Pier Andrea Borea

Dipartimento di Medicina Clinica e Sperimentale-Sezione di Farmacologia, Università di Ferrara, 44100 Ferrara, Italy

Preferred Abstract (Original):

A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives has been identified as potent A(2B) adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A(2B), A(1), A(2A), and A(3) adenosine receptors. N-(4-chloro-phenyl)-2-[3-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-5-methyl-pyrazol-1-yl] (11c) showed a high affinity for the human A(2B) adenosine receptor K(i)=7nM and good selectivity (A(1), A(2A), A(3)/A(2B)>140). Synthesis and SAR of this novel class of compounds is presented herein.