Bioisosterism Definition:
- Bioisosterism are structurally similar chemical groups that mimic the biological activity of another.
Importance in Drug Design:
- Improved Activity: Replacement of groups can enhance potency and reduce toxicity.
- Increased Stability: Bioisosteres improve metabolic stability.
- Reduced Side Effects: Modification helps improve drug safety.
Examples:
- Sulfonamide (-SO₂NH₂) as a bioisostere of carboxyl (-COOH) in diuretics.
- Fluorine (F) in fluoroquinolones for increased metabolic stability.
Types of Bioisosterism:
- Classical Bioisosteres: Atoms or groups with similar sizes and electronic properties (e.g., replacing a hydrogen atom with a fluorine atom).
- Non-Classical Bioisosteres: Groups that may not be similar in size or shape but mimic the biological properties of the original group.
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