Biological properties of 1 2 benzisothiazole derivatives local anesthetic activity of some bz alkylaminoacylamino 1 2 benzisothiazoles

Amoretti, L.; Zappia, L.

Ateneo Parmense Acta Naturalia 13(1): 3-16


Accession: 004838320

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A new group of 5- and 7-(alkylaminoacyl)amino-3-methoxy-1,2-benzisothiazoles were prepared and tested for their local anesthetic properties. The compounds were obtained from 5- and 7-amino-3-methoxy-1,2-benzisothiazole by acylation with aloalkanoylchloride. From these adducts were prepared the amides by reaction with the required alkylamine. The local anesthetic activity of the compounds, isolated as hydrochlorides, was tested in 3 biological preparations designed to show the activity of the compounds in infiltration anesthesia, in surface anesthesia and conduction anesthesia. Most of new 7-benzisotiazole amides proved active in infiltration anesthesia, mildly toxic and resistant to hydrolyzing agents.