Nonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials
Edwin G. Tse, Sevan D. Houston, Craig M. Williams, G. Paul Savage, Louis M. Rendina, Irene Hallyburton, Mark Anderson, Raman Sharma, Gregory S. Walker, R. Scott Obach, Matthew H. Todd
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.
Topics & Concepts
BioisostereCubaneChemistryStereochemistryMetabolic stabilityCombinatorial chemistryLead compoundMoleculeIn vitroChemical synthesisOrganic chemistryBiochemistrySynthesis and Catalytic ReactionsHIV/AIDS drug development and treatmentPharmacological Receptor Mechanisms and Effects