119139-23-0, Name is 3,4-Di(1H-indol-3-yl)-1H-pyrrole-2,5-dione, belongs to chiral-nitrogen-ligands compound, is a common compound. 119139-23-0In an article, authors is Arbuckle, William, once mentioned the new application about 119139-23-0.
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist
The previously described lead compound 5 is a potent and selective V 1A antagonist with affinity at both the rat and human receptor, but displays poor oral bioavailability and moderate clearance. We report herein the successful optimisation of the pharmacokinetic (PK) properties to afford the potent, selective, orally bioavailable and CNS penetrant compound 15f. A custom optimisation approach was required which demonstrated the value of using early, rapid in vivo PK studies to show improvements in oral exposure. Such assays may be of particular value where low oral bioavailability is anticipated to be multifactorial (e.g., permeability, gut wall metabolism and/or transport) where satisfactory modelling of in vitro data is likely to be difficult within a drug discovery context.
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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis