Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 19, Pages 6153-6157Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm900796p
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Funding
- ESTEVE, Barcelona, Spain [FBG2004/05-302663, FBG2006/07-303647]
- Fundacio Bosch i Gimpera-Universitat de Barcelona, Spain
- AGAUR
- Grup de Recerca Consolidat [2005SGR158, 2009SGR562]
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Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellent binding affinities and an antagonistic response at the 5-HT6 receptor, with K-i and IC50 values in the nanomolar range (K-i >= 1.2 nM, IC50 >= 47 nM, and I-max <= 173%).
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