BIOISOSTERISM PDF

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Bioisosterism: A Useful Strategy for Molecular Modification and Drug Design

In medicinal chemistry , bioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another chemical compound. In drug design , [1] the purpose of exchanging one bioisostere for another is to enhance the desired biological or physical properties of a compound without making significant changes in chemical structure. The main use of this term and its techniques are related to pharmaceutical sciences. Bioisosterism is used to reduce toxicity, change bioavailability , or modify the activity of the lead compound, and may alter the metabolism of the lead. Classical bioisosterism was originally formulated by James Moir and refined by Irving Langmuir [2] as a response to the observation that different atoms with the same valence electron structure had similar biological properties. For example, the replacement of a hydrogen atom with a fluorine atom at a site of metabolic oxidation in a drug candidate may prevent such metabolism from taking place.

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