Work

Discovery, synthesis and structure–activity analysis of symmetrical 2,7-disubstituted fluorenones as urea transporter inhibitors

Year: 2015

Type: article

Abstract: ~ 1 μM. Analysis of in vitro metabolic stability in hepatic microsomes indicated metabolism of 2,7-disubstituted fluorenones by reductase and subsequent elimination. Computational docking to a homology model of UT-A1 suggested UT inhibitor binding to the UT cytoplasmic domain at a site that does not overlap with the putative urea binding site.

Source: MedChemComm

DOI: 10.1039/c5md00198f

Authors: Sujin Lee, Cristina Esteva-Font, Puay-Wah Phuan, Marc O. Anderson, A. S. Verkman

Institutions: University of California, San Francisco, University of California System, San Francisco State University

Language: English

Topic: Synthesis and biological activity

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: green

Funders: National Institutes of Health, National Eye Institute, National Institute of Diabetes and Digestive and Kidney Diseases, National Institute of Biomedical Imaging and Bioengineering