| Literature DB >> 21186123 |
Dong Xiao1, Anandan Palani, Michael Sofolarides, Ying Huang, Robert Aslanian, Henry Vaccaro, Liwu Hong, Brian McKittrick, Robert E West, Shirley M Williams, Ren-Long Wu, Joyce Hwa, Christopher Sondey, Jean Lachowicz.
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. Copyright ÂEntities:
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Year: 2010 PMID： 21186123 DOI： 10.1016/j.bmcl.2010.11.065
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823