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A number of methods to improve the passive permeability of a set of cyclic peptides have been investigated using 6- and 7-mer macrocyclic templates. In many cases the peptides were designed by molecular dynamics calculations to evaluate the methods. The aim of this study was not only to improve passive permeability, but also to balance permeability with other physicochemical properties with the goal...
Improved understanding of the concentration of a potential drug molecule at the site of action in physiologically relevant cells or tissues has emerged as a key challenge in the early stages of drug discovery. Improved ability to carry out such studies with label-free methodology has the potential to improve understanding of drug uptake and trafficking and thus contribute to the reduction of rates...
Various situations are explored in which the nickel(0)-catalyzed enyne–epoxide reductive coupling was utilized to access key intermediates toward the total synthesis of (−)-cyatha-3,12-diene (1). Enantioenriched 3,5-dien-1-ols with a variety of functionality were obtained in a straightforward manner from easily accessible 1,3-enynes and terminal epoxides.
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