The position of the new water solubilising group will depend on the reactivity of the lead compound and the position of its pharmacophore. Initially, the former requires a general appraisal of the chemistry of the functional groups found in the lead compound. For example, if the lead structure contains aromatic ring systems it may undergo electrophilic substitution in these ring systems whilst aldehyde groups are susceptible to oxidation reduction, nucleophilic addition and condensation. This general reactivity must be taken into account when selecting a method to introduce a water solubilising group.
In order to preserve the type of activity exhibited by the lead compound, the water solubilising group should be attached to a part of the structure that is not involved in the drug-receptor interaction. Consequently, the route used to introduce a new water solubilising group and its position in the lead structure will depend on the relative reactivities of the pharmacophore and the rest of the molecule. The reagents used to introduce the new water solubilising group should be chosen on the basis that they do not react with, or in close proximity to, the pharmacophore. This will reduce the possibility of the new group affecting the relevant drug-receptor interactions.
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