Synthesis of benzo[1,2-d;3,4-d′]diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A2A receptor antagonists

Giovanni Piersanti; Luca Giorgi; Francesca Bartoccini; Giorgio Tarzia; Patrizia Minetti; Grazia Gallo; Fabrizio Giorgi; Massimo Castorina; Orlando Ghirardi; Paolo Carminati

doi:10.1039/B707599E

Synthesis of benzo[1,2-d;3,4-d′]diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A_2A receptor antagonists

Giovanni Piersanti,*^a Luca Giorgi,^a Francesca Bartoccini,^a Giorgio Tarzia,^a Patrizia Minetti,*^b Grazia Gallo,^b Fabrizio Giorgi,^b Massimo Castorina,^b Orlando Ghirardi^b and Paolo Carminati^b

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^a Institute of Medicinal Chemistry, University of Urbino “Carlo Bo”, Piazza del Rinascimento 6, 61029 Urbino (PU), Italy
E-mail: giovanni.piersanti@uniurb.it
Fax: +39 (0)722 303313
Tel: +39 (0)722 303325

^b Department of Chemistry and Department Central and Periferic Nervous System Sigma-Tau, Via Pontina Km 30,400, 00040 Pomezia, (Roma, Italy)
E-mail: Patrizia.Minetti@sigma-tau.it
Fax: +39 (0)6 91393638
Tel: +39 (0)6 91393906

Abstract

The synthesis and the binding affinity for the putative adenosine receptor antagonist 6-methyl-7-[1,2,3]triazol-2-yl-1,6-dihydrobenzo[1,2-d;3,4-d′]diimidazole (10) and 5-oxazol-2-yl-1H-pyrazolo[4,3-b]pyridin-3-ylamine (16) are reported. The title compounds were prepared from commercially available 1-chloro-2,4-dinitrobenzene (1) and 2-chloro-6-methoxy-3nitropyridine (11), respectively, but proved devoid of affinity for the adenosine A₁ and A_2A receptors.

Organic & Biomolecular Chemistry

Synthesis of benzo[1,2-d;3,4-d′]diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A_2A receptor antagonists

Abstract

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Synthesis of benzo[1,2-d;3,4-d′]diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A_2A receptor antagonists

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