Extensive structure-activity relationship studies of a series derived from atropisomer 1, a previously described chiral benzodiazepine sulfonamide series, led to a potent, brain penetrant and selective compound with excellent preclinical pharmacokinetic across species. We also describe the utilization of a high throughput mouse pharmacodynamic assay which allowed for expedient assessment of pharmacokinetic and brain distribution.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4025675 | PMC |
| http://dx.doi.org/10.1021/ml200304j | DOI Listing |
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