Discovery of pyrazoles as novel FPR1 antagonists

Andrew D Morley; Andrew Cook; Sarah King; Bryan Roberts; Sarah Lever; Richard Weaver; Cathy Macdonald; John Unitt; Malbinder Fagura; Tim Phillips; Richard Lewis; Mark Wenlock

doi:10.1016/j.bmcl.2011.08.085

Discovery of pyrazoles as novel FPR1 antagonists

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6456-60. doi: 10.1016/j.bmcl.2011.08.085. Epub 2011 Sep 6.

Authors

Andrew D Morley¹, Andrew Cook, Sarah King, Bryan Roberts, Sarah Lever, Richard Weaver, Cathy Macdonald, John Unitt, Malbinder Fagura, Tim Phillips, Richard Lewis, Mark Wenlock

Affiliation

¹ AstraZeneca R&D Charnwood, Chemistry, Bakewell Road, Loughborough LE11 5RH, UK. andymorley@live.com

PMID: 21955939
DOI: 10.1016/j.bmcl.2011.08.085

Abstract

A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in vitro DMPK profiles to be of further interest.

MeSH terms

Drug Discovery
Humans
Neutrophils / drug effects
Pyrazoles / chemistry
Pyrazoles / pharmacology*
Receptors, Formyl Peptide / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Pyrazoles
Receptors, Formyl Peptide