64318-33-8Relevant academic research and scientific papers
Synthesis of 5-iodo-1,2,3-triazole-containing macrocycles using copper flow reactor technology
Bogdan, Andrew R.,James, Keith
supporting information; experimental part, p. 4060 - 4063 (2011/09/21)
A new macrocyclization strategy to synthesize 12- to 31-membered 5-iodo-1,2,3-triazole-containing macrocycles is described. The macrocycles have been generated using a simple and efficient copper-catalyzed cycloaddition in flow under environmentally frien
Comparison of diffusion coefficients for matched pairs of macrocyclic and linear molecules over a drug-like molecular weight range
Bogdan, Andrew R.,Davies, Nichola L.,James, Keith
supporting information; experimental part, p. 7727 - 7733 (2011/12/03)
The diffusion coefficients of a series of closely matched pairs of macrocyclic and linear molecules have been compared using NMR spectroscopy. The macrocyclic series was designed both to overlap with and extend beyond the molecular weight range typically employed for drug-like molecules. The linear molecules each represent a carbogenic fission of their macrocyclic counterparts, designed to minimize differences in functionality and physicochemical properties. Each series of molecules was prepared using copper catalyzed azide-alkyne cycloaddition (CuAAC) reactions conducted in a flow using a copper tube. The macrocyclic series exhibited consistently higher diffusion across the entire molecular weight range studied. The fold difference in diffusion coefficients between the macrocyclic and linear analogues appeared to be independent of either solvent viscosity or dielectric environment.
Structure-activity relationship studies of a bisbenzimidazole-based, Zn2+-dependent inhibitor of HCV NS3 serine protease
Yeung, Kap-Sun,Meanwell, Nicholas A.,Qiu, Zhilei,Hernandez, Dennis,Zhang, Sharon,McPhee, Fiona,Weinheimer, Steve,Clark, James M.,Janc, James W.
, p. 2355 - 2359 (2007/10/03)
A survey of isosteric replacements of the phosphonoalanine side chain coupled with a process of conformational constraint of a bisbenzimidazole-based, Zn2+-dependent inhibitor of hepatitis C virus (HCV) NS3 serine protease resulted in the identification of novel series of active compounds with extended side chains. However, Zn2+-dependent HCV NS3 inhibition was relatively insensitive to the structural variations examined but dependent on the presence of negatively charged functionality. This result was interpreted in the context of an initial electrostatic interaction between protease and inhibitor that is subsequently consolidated by Zn2+, with binding facilitated by the featureless active site and proximal regions of the HCV NS3 protein.
Immunoassay for pharmacologically active phenethylamines
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, (2008/06/13)
New hapten compositions useful in preparing antigens which may be employed in eliciting antibodies useful in an improved radioimmunoassay for pharmacologically active phenethylamines are disclosed. Particular phenethylamins which are preferably detected b
