Bioisosteres are chemical substituents, groups, atoms, or moieties that have
similar physical and chemical properties, producing analogous biological effects but
with greater impact and potency. Bioisostere replacement is an impactful concept in
medicinal chemistry. Bioisostere replacement is used for attenuation of toxicity,
enhancement of the activity of the lead compound, or alterations in pharmacokinetics
and toxicity of the lead. This chapter deals with the degradation or minimization of
ecotoxic waste through bioisostere replacement. The chapter details bioisosteric
replacements for the degradation of eco-hazardous wastes in two ways, i.e., direct way
and indirect way. The direct way involves bioisosteric changes in insecticides, which
directly affects the environment, while the indirect way involves bioisosteric
modifications in drug molecules to increase their bioavailability and half-life period so
that maximum drug is consumed within the body, providing better efficacy against the
disease and release of a minimum amount of waste into the environment. These
modifications prove to be eco-friendly. Some important bioisosteric groups used for
replacement are -fluoro, -deutero, -nitro, -t-butyl, and others. This chapter gives an
insight into the plausible alterations with improved functional groups in bioisosterism
to improve the eco-detrimental effects of compounds or drugs.
Keywords: Bioisosteres, Drugs, Ecofriendly, Half-life period, Insecticides,
Medicinal chemistry, Metabolites.
