- Synthesis of benzo[1,2-d;3,4-d′]diimidazole and 1H-pyrazolo[4,3-b] pyridine as putative A2A receptor antagonists
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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 A2A receptors. The Royal Society of Chemistry.
- Piersanti, Giovanni,Giorgi, Luca,Bartoccini, Francesca,Tarzia, Giorgio,Minetti, Patrizia,Gallo, Grazia,Giorgi, Fabrizio,Castorina, Massimo,Ghirardi, Orlando,Carminati, Paolo
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p. 2567 - 2571
(2008/03/14)
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- Quinazoline and benzimidazole MCH-1R antagonists
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We have modified the previously reported 2-aminoquinoline 1 to provide two novel series of MCH-1R antagonists. Representative compounds from the quinazoline and benzimidazole series have been shown to be potent and selective, with promising in vitro eADME profiles.
- Arienzo, Rosa,Cramp, Sue,Dyke, Hazel J.,Lockey, Peter M.,Norman, Dennis,Roach, Alan G.,Smith, Phil,Wong, Melanie,Wren, Stephen P.
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p. 1403 - 1407
(2007/10/03)
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- BICYCLIC COMPOUNDS AND THEIR THERAPEUTIC USE
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Compounds of the formula (1) are useful as MCH mediator, and in the therapy of obesity.
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Page/Page column 53-54
(2010/02/11)
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- Pyridinium Betaines Derived from Thiazolo and Imidazoacridinones
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Four betaines derived from imidazo[4,5-a], imidazo[5,4-a] and thiazolo[5,4-a]acridine have been prepared in a six step procedure starting from 2-chlorobenzimidazoles and benzothiazoles. The 1H and 133C nmr has been used to characteri
- Galy, Jean-Pierre,Hanoun, Jean-Pierre,Pique, Valerie,Jagerovic, Nadine,Elguero, Jose
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p. 1781 - 1787
(2007/10/03)
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