Abstract
The electronic properties and relatively small size of fluorine
endow it with considerable versatility as a bioisostere
and it has found application as a substitute for lone pairs of electrons,
the hydrogen atom, and the methyl group
while also acting as a functional mimetic of the carbonyl,
carbinol, and nitrile moieties.
In this context, fluorine substitution can influence the potency,
conformation, metabolism, membrane permeability,
and P-gp recognition of a molecule and temper inhibition
of the hERG channel by basic amines.
However, as a consequence of the unique properties of fluorine,
it features prominently in the design of higher order structural metaphors
that are more esoteric in their conception and
which reflect a more sophisticated molecular construction
that broadens biological mimesis.
In this Perspective, applications of fluorine in the construction of bioisosteric elements designed to enhance the in vitro and in vivo properties of a molecule are summarized.
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