Journal of Medicinal Chemistry · 2020 · 149 citations · 44 references
PharmacyMedicinal ChemistryPharmacologyBioisosterismDrug DiscoveryMetabolismAromatic BioisosteresBioisosteric DesignBioisosteric ReplacementMetabolic Stability EnhancementMetabolic Stability OptimizationNonclassical BioisosteresAntimalarial AgentsAntimalarial ChemotherapyAntimalarial Drug DevelopmentBioisosteric OptimizationMetabolic Stability ModulationNonclassical BioisosterismPhenyl ReplacementPlasmodium Falciparum
) 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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Antonia F. Stepan, Chakrapani Subramanyam, Ivan Efremov et al. · Journal of Medicinal Chemistry · 2012 · 446 citations · Full text