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Bioorg Med Chem Lett. 2010 Sep 1;20(17):5241-4. doi: 10.1016/j.bmcl.2010.06.138. Epub 2010 Jul 24.

Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.

Author information

1
Medicinal Chemistry Research, H. Lundbeck A/S, Valby, Denmark. anette.sams@leo-pharma.com

Abstract

Herein we describe the discovery of a series of novel adenosine A(2A) receptor antagonists. A successful hit-to-lead optimization of an HTS hit led to replacement of a metabolically labile ester moiety with a heteroaromatic group. A compound from the series, (cyclopropanecarboxylic acid [5-(5-methyl-[1,2,4]oxadiazol-3-yl)-4-phenyl-thiazol-2-yl]-amide, compound 13), was shown to be effective in reversing haloperidol-induced hypolocomotion, a model of motor dysfunction in Parkinson's Disease.

PMID:
20659802
DOI:
10.1016/j.bmcl.2010.06.138
[Indexed for MEDLINE]

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