Ch2-3F110 - Chapter 2 (Cont.) Drug Discovery, Design and...

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Chapter 2 (Cont.) Drug Discovery, Design and Development
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D. Modifications Drugs must be chemically stable in aqueous solutions Some drugs have functional groups which are easily hydrolyzed in the stomach.
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i) Steric shields -adding a bulky alkyl group to hinder the approaching enzyme
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ii) Isoteres -chemical group replacing another group to stabilize functional group without affecting activity
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Isoteres (cont.) Actually use bioisoteres -size and electronic factors aren’t as important as biological activity -similar chemical, physical and biological properties
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Isosteres (cont.) Classical isosteres: same number of valence electrons, but may have different number of atoms Nonclassical isosteres: do not have the same number of atoms, but have a similar biological activity
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Example celecoxib (Celebrex) much longer lasting non-steroidal anti-inflammatory drug (NSAID)
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Example ezetemibe (Zetia) much less toxic Cholesterol absorption inhibitor
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iii) Stereoelectronic stabilization steric hindrance + electronic stabilization
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This note was uploaded on 10/20/2011 for the course CHEM 4332 taught by Professor Whitlock during the Spring '11 term at Georgia Southern University .

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Ch2-3F110 - Chapter 2 (Cont.) Drug Discovery, Design and...

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