Two sets of benzotriazinone and benzoyltriazole derivs. were prepd. and tested for local anesthetic activity in comparison with lidocaine. Several of the prepd. compds. exhibited a fairly good activity comparable or superior to that of lidocaine. The presence of a benzotriazinone or a benzoyltriazole moiety as an arom. system was quite profitable for both the intensity and duration of activity. The acute toxicity in mice of the four most potent compds. of the series was also assessed. Compd. I, which has an anesthetic activity comparable to that of lidocaine, was also characterized by a more favorable therapeutic index. All compds. were tested in vitro to evaluate their neg. chronotropic action in isolated rat right atria.

Preparation and local anesthetic activity of benzotriazinone and benzoyltriazole derivatives / Caliendo, Giuseppe; Fiorino, Ferdinando; Grieco, Paolo; Perissutti, Elisa; Santagada, Vincenzo; Meli, Rosaria; MATTACE RASO, Giuseppina; Zanesco, A; De Nucci, G.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 34:12(1999), pp. 1043-1051.

Preparation and local anesthetic activity of benzotriazinone and benzoyltriazole derivatives.

CALIENDO, GIUSEPPE;FIORINO, FERDINANDO;GRIECO, PAOLO;PERISSUTTI, ELISA;SANTAGADA, VINCENZO;MELI, ROSARIA;MATTACE RASO, GIUSEPPINA;
1999

Abstract

Two sets of benzotriazinone and benzoyltriazole derivs. were prepd. and tested for local anesthetic activity in comparison with lidocaine. Several of the prepd. compds. exhibited a fairly good activity comparable or superior to that of lidocaine. The presence of a benzotriazinone or a benzoyltriazole moiety as an arom. system was quite profitable for both the intensity and duration of activity. The acute toxicity in mice of the four most potent compds. of the series was also assessed. Compd. I, which has an anesthetic activity comparable to that of lidocaine, was also characterized by a more favorable therapeutic index. All compds. were tested in vitro to evaluate their neg. chronotropic action in isolated rat right atria.
1999
Preparation and local anesthetic activity of benzotriazinone and benzoyltriazole derivatives / Caliendo, Giuseppe; Fiorino, Ferdinando; Grieco, Paolo; Perissutti, Elisa; Santagada, Vincenzo; Meli, Rosaria; MATTACE RASO, Giuseppina; Zanesco, A; De Nucci, G.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 34:12(1999), pp. 1043-1051.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/342854
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 44
  • ???jsp.display-item.citation.isi??? 42
social impact