Nonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials
Edwin G. Tse(The University of Sydney), Sevan D. Houston(The University of Queensland), Craig M. Williams(The University of Queensland), G. Paul Savage(CSIRO Manufacturing), Louis M. Rendina(The University of Sydney), Irene Hallyburton(University of Dundee), Mark Anderson(University of Dundee), Raman Sharma(Pfizer (United States)), Gregory S. Walker(Pfizer (United States)), R. Scott Obach(Pfizer (United States)), Matthew H. Todd(University College London)
Cited by 145Open Access
Abstract
) was found to be equipotent to its parent phenyl compound and showed significantly improved metabolic properties. While these results demonstrate the utility of these atypical bioisosteres when used in a medicinal chemistry program, the search to find a suitable bioisostere may well require the preparation of many candidates, in our case, 32 compounds.
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