SAR of Sulphonylureas

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Chapter: Medicinal Chemistry : Oral Hypogylcaemic Drugs

The benzene ring should contain a substitutent preferably in the para position. The substituents, such as methyl, acetyl, amino, chloro, bromo, trifluoro methyl, and dithiomethyl were found to enhance the antihyperglycaemic activity.


SAR of Sulphonylureas


1.           The benzene ring should contain a substitutent preferably in the para position. The substituents, such as methyl, acetyl, amino, chloro, bromo, trifluoro methyl, and dithiomethyl were found to enhance the antihyperglycaemic activity.

2.           When the para position of benzene is substituted with aryl carboxamidoalkyl group (second-generation sulphonylureas, such as glibenclamide) the activity was found to be enhanced further.

3.           The size of the group attached to the terminal nitrogen is crucial for activity. The group should also impart lipophilicity to the compound N-methyl and ethyl substituents that show no activity, whereas N-propyl and higher homologues were found to be active and the activity is lost when the N-substituent contains 12 or more carbons.

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