Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371104 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
A series of 2-piperidinopiperidine-5-arylthiadiazoles was synthesized and subjected to a structure–activity relationship (SAR) investigation. The potency of this series was improved to the single digit nanomolar range. The key analogs were shown to be free of P450 issues, and they also maintained good ex vivo activity and brain penetration.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Dong Xiao, Anandan Palani, Michael Sofolarides, Ying Huang, Robert Aslanian, Henry Vaccaro, Liwu Hong, Brian McKittrick, Robert E. West Jr., Shirley M. Williams, Ren-Long Wu, Joyce Hwa, Christopher Sondey, Jean Lachowicz,