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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Authors: | Horchler Carey L McCauley John P Hall James E Snyder Dean H Craig Moore W Hudzik Thomas J Chapdelaine Marc J |
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Affiliation: | CNS Chemistry and Neuroscience, AstraZeneca Pharmaceuticals LP, 1800 Concord Pike, Wilmington, DE 19850, USA. carey.horchler@astrazeneca.com |
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Abstract: | Multiparallel amenable syntheses of 6-methoxy-8-amino-4-oxo-1,4-dihydroquinoline-2-carboxylic acid-(4-morpholin-4-yl-phenyl)amides (I) and 4-amino-6-methoxy-8-(4-methyl-piperazin-1-yl)-quinoline-2-carboxylic acid (4-morpholin-4-yl-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. |
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