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Bioorg Med Chem. 2006 Apr 1;14(7):2358-65. Epub 2005 Nov 28.

2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers.

Author information

1
Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, 381 Royal Parade, Parkville, Vic. 3052, Australia.

Abstract

Three series of 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene and 2-amino-5,6,7,8-tetrahydrocyclohepta[b]thiophenes with 3-carboxylates and carboxamides have been prepared using the Gewald synthesis and evaluated as A(1)AR allosteric enhancers. The structure-activity relationships of these classes of compound are described. A number of compounds, notably 7b, are more potent and efficacious than PD81,723 (1).

PMID:
16314104
DOI:
10.1016/j.bmc.2005.11.018
[Indexed for MEDLINE]

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