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Travis
Lv 4
Travis asked in Science & MathematicsChemistry · 1 decade ago

In drug design, how does the incorporation of halogen increase its stability?

does it have to do with lipophilicity/hydrophilicity?

Update:

Or how does it increase its lipophilicity?

2 Answers

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  • Anonymous
    1 decade ago
    Favorite Answer

    The most typical reason why halogens (esp F) are incorporated into drug candidate molecules (usually replacing a proton on an aromatic ring, for example) has to do with metabolism. Oxidation of compounds is one pathway by which the body begins metabolizing drug substances; hydrogens are frequently one spot where oxidation occurs. In replacing key protons with halogens, that oxidation pathway is generally shut down -- allowing the original drug substance to survive longer as such in the body, and therefore have longer period of time to have the desired clinical effect.

    Source(s): PhD organic chemistry (and pharmaceutical chemist)
  • 1 decade ago

    there could be free radicals (substances lacking one electron) in those drugs, and since halogens have 7 valence electrons, they would react with the free radicals, taking the latter's extra electrons with them

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