Synthesis of novel quinolone and quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl)amides:: A late-stage diversification approach to potent 5HT1B antagonists

Synthesis of novel quinolone and quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl)amides:: A late-stage diversification approach to potent 5HT1B antagonists
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DOI:
10.1016/j.bmc.2006.10.037
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发表时间:
2007-01-15
影响因子:
3.5
通讯作者:
Chapdelaine, Marc J.
Chapdelaine, Marc J.
中科院分区:
医学3区
文献类型:
--
作者:
Horchler, Carey L.;McCauley, John P., Jr.;Chapdelaine, Marc J.

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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.