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,

Journal of Medicinal Chemistry · 2020 · 149 citations · 44 references

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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.

References

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