58965-42-7Relevant articles and documents
Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor
Favia, Angelo D.,Habrant, Damien,Scarpelli, Rita,Migliore, Marco,Albani, Clara,Bertozzi, Sine Mandrup,Dionisi, Mauro,Tarozzo, Glauco,Piomelli, Daniele,Cavalli, Andrea,De Vivo, Marco
, p. 8807 - 8826,20 (2020/09/16)
Pain and inflammation are major therapeutic areas for drug discovery. Current drugs for these pathologies have limited efficacy, however, and often cause a number of unwanted side effects. In the present study, we identify the nonsteroidal anti-inflammatory drug carprofen as a multitarget-directed ligand that simultaneously inhibits cyclooxygenase-1 (COX-1), COX-2, and fatty acid amide hydrolase (FAAH). Additionally, we synthesized and tested several derivatives of carprofen, sharing this multitarget activity. This may result in improved analgesic efficacy and reduced side effects (Naidu et al. J. Pharmacol. Exp. Ther.2009, 329, 48-56; Fowler, C. J.; et al. J. Enzyme Inhib. Med. Chem.2012, in press; Sasso et al. Pharmacol. Res.2012, 65, 553). The new compounds are among the most potent multitarget FAAH/COX inhibitors reported so far in the literature and thus may represent promising starting points for the discovery of new analgesic and anti-inflammatory drugs.
CORRELATION BETWEEN THE STRUCTURE AND ACTIVITY OF AMINOSTIGMINE DERIVATIVES CONTAINING VARIOUS SUBSTITUENTS AT THE NITROGEN ATOM OF THE CARBAMOYL GROUP
Prozorovskii, V. B.,Pavlova, L. V.,Suslova, I. M.,Belozerova, L. V.,Kokushkina, A. V.,Sazonova, A. V.
, p. 589 - 593 (2007/10/03)
Sixteen aminostigmine derivatives containing various substituents at the nitrogen atom of the carbamoyl group have been prepared, and their anticholine esterase activity in vitro, ionization constants, hydrophobicity, and toxicity have been determined.
