Preparation and local anaesthetic activity of benzotriazinone and benzoyltriazole derivatives

Two sets of benzotriazinone and benzoyltriazole derivatives were prepared a nd tested for local anaesthetic activity in comparison with lidocaine. Seve ral of the prepared compounds exhibited a fairly good activity comparable o r superior to that of Lidocaine. The presence of a benzotriazinone or a ben zoyltriazole moiety as an aromatic system was quite profitable for both the intensity and duration of activity. The acute toxicity in mice of the four most potent compounds of the series was also assessed. Compound Ib, which has an anaesthetic activity comparable to that of lidocaine, was also chara cterized by a more favourable therapeutic index. All compounds were tested in vitro to evaluate their negative chronotropic action in isolated rat rig ht atria. (C) 1999 Editions scientifiques et medicales Elsevier SAS.