Ontology highlight
ABSTRACT:
SUBMITTER: Liu Y
PROVIDER: S-EPMC3954708 | biostudies-literature | 2013 Jun
REPOSITORIES: biostudies-literature
Liu Y Y Esteva-Font C C Yao C C Phuan P W PW Verkman A S AS Anderson M O MO
Bioorganic & medicinal chemistry letters 20130401 11
The kidney urea transport protein UT-B is an attractive target for the development of small-molecule inhibitors with a novel diuretic ('urearetic') action. Previously, two compounds in the triazolothienopyrimidine scaffold (1a and 1c) were reported as UT-B inhibitors. Compound 1c incorporates a 1,1-difluoroethyl group, which affords improved microsomal stability when compared to the corresponding ethyl-substituted compound 1a. Here, a small focused library (4a-4f) was developed around lead inhib ...[more]