Abstract
A series of substituted benzylamines 2-48 were prepared as part of a strategy to identify structurally differentiated and synthetically more accessible selective serotonin reuptake inhibitors, relative to clinical candidate 1. In particular, 44 and 48; demonstrated low nanomolar potency and good selectivity, in a structurally simplified template and, in vivo, very low Vdu, significantly lower than l, and a more rapid T(max), consistent with our clinical objectives.
MeSH terms
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Benzylamines / chemistry*
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Inhibitory Concentration 50
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Kinetics
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Models, Chemical
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Molecular Conformation
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Receptors, Serotonin / metabolism
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Selective Serotonin Reuptake Inhibitors / chemical synthesis*
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin / chemistry
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Serotonin / metabolism
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Structure-Activity Relationship
Substances
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Benzylamines
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Receptors, Serotonin
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Serotonin Uptake Inhibitors
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Serotonin