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