Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT(7) antagonists |
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Authors: | Rudolph Dale A Dvorak Curt A Dvorak Lisa Nepomuceno Diane Bonaventure Pascal Lovenberg Timothy W Carruthers Nicholas I |
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Affiliation: | Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States |
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Abstract: | The synthesis and SAR for a novel series of tetrahydropyrido[3,2-c]pyrroles is described. Optimization of the pendant aryl ring lead to high binding affinity at the 5-HT7 receptor when small lipophilic groups were placed in the para position. Modification of the N-benzyl group and secondary amine were not well tolerated. A representative set of compounds was shown to be functional antagonists of the 5-HT7 receptor. |
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Keywords: | 5-HT7 5-HT7 receptor Serotonin |
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