Pfizer Inc
Medicinal chemistry
... of a Series of 1, 3, 4-Trisubstituted Pyrrolidines Jeffrey A. Stafford,* Nicole L. Valvano, Paul L. Feldman, E. Sloan Brawley, David J. Cowan, Paul L. Domanico, Michael A. Leesnitzer, Dudley A. Rose ... John, T.; Steiner, B.; Rodgers,... more
A novel series of diazepine-based hydroxamic acid inhibitors of MMP-1, MMP-9, and MMP-13 were prepared and evaluated both in vitro and in vivo.
Due to the high attrition rate of central nervous system drug candidates during clinical trials, the assessment of blood-brain barrier (BBB) penetration in early research is particularly important. A genetic approximation (GA)-based... more
ABSTRACT A series of modifications were made to the C-3 substituent of the 1,5-benzodiazepine CCK-A agonist 1. Replacement of the inner urea NH and addition of a methyl group to generate a C-3 quaternary carbon resulted in acetamide 6,... more
We previously described a series of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepine CCK-A agonists exemplified by compound 1 (GW 5823), which is the first reported binding selective CCK-A full agonist demonstrating oral efficacy in a rat... more