title: Optimisation of a pyrazole series of progesterone antagonists; Part 1.
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.
authors.affiliation: Department of World-Wide Medicinal Chemistry, Pfizer PharmaTherapeutics Division, Sandwich CT 13 9NJ, UK. kevin.dack@pfizer.com
authors.forename: Kevin N
authors.initials: KN
authors.lastname: Dack
authors.forename: Sarah
authors.initials: S
authors.lastname: Skerratt
authors.forename: Patrick S
authors.initials: PS
authors.lastname: Johnson
authors.forename: Paul A
authors.initials: PA
authors.lastname: Bradley
authors.forename: Ian R
authors.initials: IR
authors.lastname: Marsh
mesh_terms: D015195:Drug Design; D008024:Ligands; D008958:Models, Molecular; D011374:Progesterone / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D008024:Ligands; D011720:Pyrazoles; D011374:Progesterone