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  • Title: Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage.
    Author: Perissutti E, Fiorino F, Renner C, Severino B, Roviezzo F, Sautebin L, Rossi A, Cirino G, Santagada V, Caliendo G.
    Journal: J Med Chem; 2006 Dec 28; 49(26):7774-80. PubMed ID: 17181159.
    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.
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