Pharmacologically active sulfoximides: 5-hexyl-7-)S-methylsulfonimidoly) xanthone-2-carboxylic acid, a potent...

The antiallergic activity of some xanthone derivatives containing a sulfoximide substitutent has been investigated. While 2-(S-methylsulfonimidoyl)xanthone itself was found to be inactive, a series of 7-(S-methylsulfonimidoly)-xanthone-2-carboxylic acids showed good levels of activity in the passive cutaneous anaphylaxis screen. N-Substituted sulfoximide derivatives were, without exception, less active than the corresponding unsubstituted compounds. The activity of the 7-(S-methylsulfonimidoyl)xanthone-2-carboxylic acids could be enhanced by the introduction of an alkyl or alkoxy substituent at C-5. As a result of these studies, 5-hexyl-7(S-methylsulfonimidoyl)xanthone-2-carboxylic acid has been selected for further investigation as an antipasthmatic agent.