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  • Bioisosteric Replacements - Cambridge MedChem Consulting
    The bioisosteric replacement may be physicochemically or topologically based The replacement can attenuate toxicity, modify activity of lead, and or alter pharmacokinetics or the toxicity of the lead
  • Bioisosteric Replacement as a Tool in Anti-HIV Drug Design
    Bioisosteric replacement is a powerful tool for modulating the drug-like properties, toxicity, and chemical space of experimental therapeutics In this review, we focus on selected cases where bioisosteric replacement and scaffold hopping have been used in the development of new anti-HIV-1 therapeutics
  • Bioisostere - Wikipedia
    Bioisosterism is used to reduce toxicity, change bioavailability, or modify the activity of the lead compound, and may alter the metabolism of the lead
  • SwissBioisostere 2021: updated structural, bioactivity and . . .
    Bioisosteric replacement is a routine practice for lead optimization At this step, medicinal chemists apply numerous small modifications at the periphery of validated chemotypes to adjust properties and finally generate drug candidates (8)
  • Bioisosteres Cheat Sheet
    This article highlights some of the most common bioisosteric replacement strategies for phenyl groups, while also exploring emerging C(sp3)-rich motifs that are gaining increased attention for their potential in modern drug design
  • Classical, Non-Classical Bioisosteres and Stereochemistry
    How does changing CO2H to tetrazole in Losartan modulate metabolism? Tetrazole increases oral bioavailability due to increased lipophilicity (aromatic ring) and tetrazole increases binding affinity due to better distribution of negative charge; lower dose of drug needed for same effect





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