SAR of CAse Inhibitiors

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Chapter: Medicinal Chemistry : Diuretics

Two groups of CAse inhibitors are 1. Heterocylic sulphonamides 2. Meta-disulphamoyl benzene derivatives


SAR of CAse Inhibitiors

Two groups of CAse inhibitors are

  1. Heterocylic sulphonamides

  2. Meta-disulphamoyl benzene derivatives


1. Heterocylic sulphonamides


  • The C-2 sulphamoyl group is important for activity.

  • The free sulphamolyl moiety is necessary to bind with Zn++ in the enzyme; hence, substitution of sulphamoyl group gives inactive compound.

  • The moiety to which the sulphamoyl group is attached must be aromatic in character.

  • The heterocyclic sulphonamides with higher partition coefficient and lowest Pka value have greatest CAse inhibitory and diuretic activites. Example—acetazolamide, methazolamide.

  • N-alkylation with methyl group on ring Nof acetazolamide yields active compound (methazolamide).


2. m-Disulphamoyl benzene derivatives


  • m-Disulphamoyl benzene do not have diuretic activity.

  • Substituted m-sulphamoyl benzene exhibits diuretic activity.

  • The unsubstituted sulphamoyl moiety is essential for the activity; any substitution leads to affect the potency of the compound.

  • The sulphamoyl moiety can be replaced with similar electrophilic groups (e.g. carboxyl, carbamoyl) that may increase the potency of the compound.

  • Maximum diuretic activity is obtained when 4th is substituted by Cl, Br, CF3 or NO2 group.

  • Substitution of amino group at 6th position increases aleuronic activity, but decreases CAse inhibitor activity.

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