Optimisation of a pyrazole series of progesterone antagonists; Part 1

Kevin N Dack; Sarah Skerratt; Patrick S Johnson; Paul A Bradley; Ian R Marsh

doi:10.1016/j.bmcl.2010.04.018

Optimisation of a pyrazole series of progesterone antagonists; Part 1

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3384-6. doi: 10.1016/j.bmcl.2010.04.018. Epub 2010 Apr 13.

Authors

Kevin N Dack¹, Sarah Skerratt, Patrick S Johnson, Paul A Bradley, Ian R Marsh

Affiliation

¹ Department of World-Wide Medicinal Chemistry, Pfizer PharmaTherapeutics Division, Sandwich CT 13 9NJ, UK. kevin.dack@pfizer.com

PMID: 20430618
DOI: 10.1016/j.bmcl.2010.04.018

Abstract

The design and synthesis of a novel series of non-steroidal progesterone receptor antagonists is described. Ligand-lipophilicity efficiency (LLE) was used in the selection of a prototype agent for in vivo pharmacology studies.

MeSH terms

Drug Design
Ligands
Models, Molecular
Progesterone / antagonists & inhibitors*
Pyrazoles / pharmacokinetics
Pyrazoles / pharmacology*

Substances

Ligands
Pyrazoles
Progesterone