Issue 8, 2016
From the journal:

MedChemComm

The design, synthesis and evaluation of low molecular weight acidic sulfonamides as URAT1 inhibitors for the treatment of gout†‡

Andy Pike,*a   R. Ian Storer,*b   Robert M. Owen,b   Emma Armstrong,c   Caroline L. Benn,c   Magda Bictash,c   Kathy F. K. Cheung,f   Kathryn Costelloe,c   Emmanuel Dardennes,f   Emma Impey,c   Philip H. Milliken,d   Elisabeth Mortimer-Cassen§d  and  Hannah J. Pearcee  

* Corresponding authors

a Pharmacokinetics Dynamics and Metabolism, Pfizer Ltd, The Portway, Granta Park, Cambridge, UK
E-mail: andy.pike@pfizer.com

b Worldwide Medicinal Chemistry, Pfizer Ltd, The Portway, Granta Park, Cambridge, UK
E-mail: ian.storer@pfizer.com

c Discovery Biology, Pfizer Ltd, The Portway, Granta Park, Cambridge, UK

d Drug Safety, Pfizer Ltd, The Portway, Granta Park, Cambridge, UK

e Pharmaceutical Sciences, Research & Development, Pfizer Ltd, The Portway, Granta Park, Cambridge, UK

f Peakdale Molecular Ltd, Discovery Park House, Ramsgate Road, Sandwich, Kent, UK

Abstract

A novel series of low molecular weight and synthetically facile acidic sulfonamides that are potent and selective URAT1 inhibitors is described. Compounds 46 and 47 were identified as promising leads from in vitro pharmacology and ADME profiling and advanced to broader in vitro and in vivo PK and toxicology studies.

Graphical abstract: The design, synthesis and evaluation of low molecular weight acidic sulfonamides as URAT1 inhibitors for the treatment of gout

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Article information

DOI
https://doi.org/10.1039/C6MD00191B
Article type
Research Article
Submitted
04 Apr 2016
Accepted
03 Jun 2016
First published
08 Jun 2016

Med. Chem. Commun., 2016,7, 1572-1579

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The design, synthesis and evaluation of low molecular weight acidic sulfonamides as URAT1 inhibitors for the treatment of gout

A. Pike, R. I. Storer, R. M. Owen, E. Armstrong, C. L. Benn, M. Bictash, K. F. K. Cheung, K. Costelloe, E. Dardennes, E. Impey, P. H. Milliken, E. Mortimer-Cassen and H. J. Pearce, Med. Chem. Commun., 2016, 7, 1572 DOI: 10.1039/C6MD00191B

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