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Preparation and local anaesthetic activity of benzotriazinone and benzoyltriazole derivatives |
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| Authors: | Giuseppe Caliendo Ferdinando Fiorino Paolo Grieco Elisa Perissutti Vincenzo Santagada Rosaria Meli Giuseppina Mattace Raso Angelina Zanesco Gilberto De Nucci |
| Affiliation: | a Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli “Federico II” Via D. Montesano 49, 80131 Napoli, Italy;b Dipartimento di Farmacologia Sperimentale, Università degli Studi di Napoli “Federico II” Via D. Montesano 49, 80131 Napoli, Italy;c Cartesius Analytical Unit, Department of Pharmacology, Biomedical Sciences Institute, University of Sao Paulo, Sao Paulo, Brazil |
| Abstract: | Two sets of benzotriazinone and benzoyltriazole derivatives were prepared and tested for local anaesthetic activity in comparison with lidocaine. Several of the prepared compounds exhibited a fairly good activity comparable or superior to that of lidocaine. The presence of a benzotriazinone or a benzoyltriazole 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 1b, which has an anaesthetic activity comparable to that of lidocaine, was also characterized by a more favourable therapeutic index. All compounds were tested in vitro to evaluate their negative chronotropic action in isolated rat right atria. |
| Keywords: | benzotriazinone benzoyltriazole local anaesthetic negative chronotropic action |
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