Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
- BIAVA M.
- PORRETTA G. C.
- POCE G.
- SUPINO S.
- MANETTI F.
- FORLI .
- BOTTA M.
- PERGOLA C.
- GHELARDINI C.
- NORCINI M.
- MAKOVEC F.
- GIORDANI A.
- ANZELLOTTI P.
- CIRILLI R.
- FERRETTI R.
- GALLINELLA B.
- LA TORRE F.
- ANZINI M.
- PATRIGNANI P.
- SAUTEBIN, LIDIA
- ROSSI, ANTONIETTA
DOIAbstract
Following our previous research on anti-inflammatory drugs (NSAIDs), we report here the synthesis of chiral 1,5-diarylpyrroles derivatives that were characterized for their in vitro inhibitory effects toward cyclooxygenase (COX) isozymes. Analysis of enzymatic affinity and COX-2 selectivity led us to the selection of one compound (+/-)-10b that was further tested in vitro in the human whole blood (HWB) and in vivo for its anti-inflammatory activity in mice. The affinity data have been rationalized through docking simulations
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