Discovery of a series of potent arylthiadiazole H sub(3) antagonists

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 go...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 21; no. 2; pp. 861 - 864
Main Authors Xiao, Dong, Palani, Anandan, Sofolarides, Michael, Huang, Ying, Aslanian, Robert, Vaccaro, Henry, Hong, Liwu, McKittrick, Brian, West, Robert E, Williams, Shirley M, Wu, Ren-Long, Hwa, Joyce, Sondey, Christopher, Lachowicz, Jean
Format Journal Article
LanguageEnglish
Published 15.01.2011
Online AccessGet full text

Cover

More Information
Summary: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.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-1
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.11.065