Novel substituted 2-methyl-3-indolylacetic derivatives were synthesized and evaluated for their activity in vitro and in vivo on COX-1 and COX-2. Active compounds were screened to determine their gastrointestinal tolerability in vivo in the rat. Results showed that 3 and 4 preferentially inhibited COX-1 in vitro and in vivo. MD simulations indicated an induced fit for COX-1 but not for COX-2, probably because of a lower plasticity of the latter.
Synthesis of 2-Methyl-3-indolylacetic Derivatives as Anti-Inflammatory Agents That Inhibit Preferentially Cyclooxygenase 1 without Gastric Damage / Perissutti, Elisa; Fiorino, Ferdinando; C., Renner; Severino, Beatrice; Roviezzo, Fiorentina; Sautebin, Lidia; Rossi, Antonietta; Cirino, Giuseppe; Santagada, Vincenzo; Caliendo, Giuseppe. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - ELETTRONICO. - 49:26(2006), pp. 7774-7780. [10.1021/jm0608199]
Synthesis of 2-Methyl-3-indolylacetic Derivatives as Anti-Inflammatory Agents That Inhibit Preferentially Cyclooxygenase 1 without Gastric Damage
PERISSUTTI, ELISA;FIORINO, FERDINANDO;SEVERINO, BEATRICE;ROVIEZZO, FIORENTINA;SAUTEBIN, LIDIA;ROSSI, ANTONIETTA;CIRINO, GIUSEPPE;SANTAGADA, VINCENZO;CALIENDO, GIUSEPPE
2006
Abstract
Novel substituted 2-methyl-3-indolylacetic derivatives were synthesized and evaluated for their activity in vitro and in vivo on COX-1 and COX-2. Active compounds were screened to determine their gastrointestinal tolerability in vivo in the rat. Results showed that 3 and 4 preferentially inhibited COX-1 in vitro and in vivo. MD simulations indicated an induced fit for COX-1 but not for COX-2, probably because of a lower plasticity of the latter.| File | Dimensione | Formato | |
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