A series of phenyl piperidine alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.
To investigate the functional roles of individual HLA-DR residues in T cell recognition, transfectants expressing wild-type or mutant DR(o~, B1"0401) molecules with single amino acid substitutions at 14 polymorphic positions of the DI~1"0401 chain or 19 positions of the DRo~ chain were used as antigen-presenting cells for five T cell clones specific for the… (More)
A series of N-aryl isonipecotamide alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13.
A series of alpha-alkyl-alpha-amino-beta-sulphone hydroxamates was prepared and evaluated for potency versus MMP-2 and MMP-13, and for selectivity versus MMP-1. Low nanomolar potency was obtained with selectivity versus MMP-1 ranging from >10 to >1000. Selected compounds were orally bioavailable.
Precise data on impaired psychiatrists is lacking, but the evidence suggests significant prevalence due to mental illness, substance abuse, and personality disorder. The complexity and stress of the profession may induce and aggravate vulnerabilities that lead to impaired functioning. Although the very idea of impaired function centers on harmful patient… (More)