Medicinal chemistry Chapter 13 New Methods and Techniques
Medicinal chemistry Chapter 13 New Methods and Techniques
Prodrug The term prodrug, which was used initially by Albert Hl, is a pharmacologically inactive compound that is converted into an active drug by a metabolic biotransformation a prodrug also can be activated by a nonenzymatic process such as hydrolysis but in this case the compounds generally are inherently unstable and may cause stability problems
Prodrug • The term prodrug, which was used initially by Albert HI, is a pharmacologically inactive compound that is converted into an active drug by a metabolic biotransformation. • A prodrug also can be activated by a nonenzymatic process such as hydrolysis, but in this case the compounds generally are inherently unstable and may cause stability problems
The prodrug to drug conversion can occur before absorption, during absorption, after absorption, or at a specific site in the body In the ideal case a prodrug is converted to the drug as soon as the desired goal for designing the prodrug has been achieved
• The prodrug to drug conversion can occur before absorption, during absorption, after absorption, or at a specific site in the body. • In the ideal case a prodrug is converted to the drug as soon as the desired goal for designing the prodrug has been achieved
Soft drug Soft drugs are biologically active drugs designed to have a predictable and controllable metabolism to nontoxic and inactive products after they have achieved their desired pharmacological ettect The molecule could be deactivated and detoxified shortly after it has exerted its biological effect, the therapeutic index could be increased, providing a safer drug
Soft Drug • Soft drugs are biologically active drugs designed to have a predictable and controllable metabolism to nontoxic and inactive products after they have achieved their desired pharmacological effect. • The molecule could be deactivated and detoxified shortly after it has exerted its biological effect, the therapeutic index could be increased, providing a safer drug
Feature It has a close structural similarity to the lead; It has a meta bolically sensitive moiety built into the lead structure The incorporated metabolically sensitive spot does not affect the overall physicochemical or steric properties of the lead compound
Feature • It has a close structural similarity to the lead; • It has a metabolically sensitive moiety built into the lead structure; • The incorporated metabolically sensitive spot does not affect the overall physicochemical or steric properties of the lead compound;