Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 15, Issue 2, Pages 939-950Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.10.037
Keywords
5HT(1B) antagonist; 8-amino-4-oxo-1,4-dihydroquinoline-2-carboxylic acid amides; 4-aminoquinoline-2-carboxylic acid amide
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Multiparallel amenable syntheses of 6-methoxy-8-amino-4-oxo-1,4-dihydroquinoline-2-carboxylic acid-(4-morpholin-4yl-phenyl)amides (I) and 4-amino-6-methoxy-8-(4-methyl-piperazin-1-yl)-quinoline-2-carboxylic acid (4-morpholin-4-yi-phenyl)amides (II) which facilitate late-stage diversification at the 8-position of (I) and at the 4- and 8-positions of (II) are described. The resulting novel series were determined to contain potent 5HT(1B) antagonists. Preliminary SAR data are presented. Published by Elsevier Ltd.
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