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A new route to the anilides of 4-halogeno-3-sulphamoylbenzoic acid is described. These novel compounds, and in particular 4-chloro-2′-methyl-3-sulphamoylbenzanilide, are found to be potent orally active diuretic agents.

The condensation of some halogeno-2,4-disulphamylbenzenes with basic reagents has been examined. Some of the resulting products have been converted into 1,2,4-benzothiadiazine-1,1-dioxide derivatives. By using 2-aminopyridine in the reaction the novel azaphenthiazines (VII) were obtained.

The requirements for diuretic activity in the sulphamoylbenzoic acid series have been studied. Optimal activity is shown by 4-halogeno-3- sulphamoylbenzoic acids.

Further new variants of tolbutamide (and two new imidazolines) are described.

The preparation of 5-chloro-2,4-disulphamyltoluene, its properties and estimation in biological fluids are described.

Some 2-alkyl-3-aryl-3H-4-quinazolones (I; X = 0) have been prepared and a number of them converted into the thioquinazolones (I; X = S). A new method for the synthesis of 3-alkyl-2-aryl-3H-4-quinazolones (VI) has been developed and has been employed for the synthesis of representative derivatives. Biological study of the above compounds revealed that some of them, and in particular the 2-alkyl-3-halophenyl-3H-4-quinazolones are potent anticonvulsant agents.

The preparation of some 1-aryloxy-3-[(2-indol-3′-ylethyl)amino]propan-2-ols is described. Their biological activity was insignificant.