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Published on: November 27, 2016
Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs)
William D Schmitz1, Derek J Denhart, Allison B Brenner
1Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492-7660, USA. william.schmitz@bms.com
Abstract:
A series of N,N-dimethylhomotryptamines was prepared and their binding affinities at the serotonin transporter (SERT) were determined. Compounds possessing an electron withdrawing substituent at the C5-position of the indole nucleus were found to be potent SSRIs. Initial attempts at conformational restriction of the propylamine sidechain by incorporation of a quinuclidine bicyclic structure did not improve binding affinity at SERT.
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