Novel propanamides as fatty acid amide hydrolase inhibitors(452 views) Deplano A, Morgillo CM, Demurtas M, Bjorklund E, Cipriano M, Svensson M, Hashemian S, Smaldone G, Pedone E, Luque FJ, Cabiddu MG, Novellino E, Fowler CJ, Catalanotti B, Onnis V
Eur J Med Chem (ISSN: 0223-5234, 1768-3254, 0223-5234linking), 2017 Aug 18; 136: 523-542.
Department of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, via Ospedale 72, Cagliari I-09124, Italy., Department of Pharmacy, Universita Degli Studi di Napoli Federico II, Napoli, Italy., Department of Pharmacology and Clinical Neuroscience, Umea University, SE-901 87 Umea, Sweden., IRCCS SDN, Via Emanuele Gianturco 113, 80143 Napoli, Italy., Institute of Biostructures and Bioimaging, CNR, Naples, Italy., Departament de Nutricio, Ciencies de l'Alimentacio i Gastronomia and Institut de Biomedicina (IBUB), Facultat de Farmacia i Ciencies de l'Alimentacio, Universitat de Barcelona, Santa Coloma de Gramenet, Spain., Department of Chemical and Geological Sciences, University of Cagliari, Italy., Department of Pharmacy, Universita Degli Studi di Napoli Federico II, Napoli, Italy. Electronic address: brucatal@unina.it.,
Department of Pharmacy, Università Degli Studi di Napoli Federico II, Napoli, Italy.
IRCCS SDN, Via Emanuele Gianturco 113, 80143 Napoli, Italy.
Institute of Biostructures and Bioimaging, CNR, Naples, Italy.
Departament de Nutrició, Ciències de l'Alimentació i Gastronomia and Institut de Biomedicina (IBUB), Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona, Santa Coloma de Gramenet, Spain.
Department of Chemical and Geological Sciences, University of Cagliari, Italy.
References: Not available.
Novel propanamides as fatty acid amide hydrolase inhibitors
Fatty acid amide hydrolase (FAAH) has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol. FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does not result in the psychotropic and peripheral side effects characterizing the agonists of the cannabinoid receptors. Here we present the discovery of a novel class of profen derivatives, the N-(heteroaryl)-2-(4-((2-(trifluoromethyl)pyridin-4-yl)amino)phenyl)propanamides, as FAAH inhibitors. Enzymatic assays showed potencies toward FAAH ranging from nanomolar to micromolar range, and the most compounds lack activity toward the two isoforms of cyclooxygenase. Extensive structure-activity studies and the definition of the binding mode for the lead compound of the series are also presented. Kinetic assays in rat and mouse FAAH on selected compounds of the series demonstrated that slight modifications of the chemical structure could influence the binding mode and give rise to competitive (TPA1) or non-competitive (TPA14) inhibition modes.
Novel propanamides as fatty acid amide hydrolase inhibitors
Ciccarelli M, Sorriento D, Coscioni E, Iaccarino G, Santulli G * Adrenergic Receptors(338 views) Endocrinol Of The Heart In Health And Dis (ISSN: 9780-1280311249780128031117), 2016; N/D: 285-315. Impact Factor:0 ViewExport to BibTeXExport to EndNote
Kim YH, Shin SW, Pellicano R, Fagoonee S, Choi IJ, Kim YI, Park B, Choi JM, Kim SG, Choi J, Park JY, Oh S, Yang HJ, Lim JH, Im JP, Kim JS, Jung HC, Ponzetto A, Figura N, Malfertheiner P, Choi IJ, Kook MC, Kim YI, Cho SJ, Lee JY, Kim CG, Park B, Nam BH, Bae SE, Choi KD, Choe J, Kim SO, Na HK, Choi JY, Ahn JY, Jung KW, Lee J, Kim DH, Chang HS, Song HJ, Lee GH, Jung HY, Seta T, Takahashi Y, Noguchi Y, Shikata S, Sakai T, Sakai K, Yamashita Y, Nakayama T, Leja M, Park JY, Murillo R, Liepniece-karele I, Isajevs S, Kikuste I, Rudzite D, Krike P, Parshutin S, Polaka I, Kirsners A, Santare D, Folkmanis V, Daugule I, Plummer M, Herrero R, Tsukamoto T, Nakagawa M, Kiriyama Y, Toyoda T, Cao X, Corral JE, Mera R, Dye CW, Morgan DR, Lee YC, Lin JT, Garcia Martin R, Matia Cubillo A, Lee SH, Park JM, Han YM, Ko WJ, Hahm KB, Leontiadis GI, Ford AC, Ichinose M, Sugano K, Jeong M, Park JM, Han YM, Park KY, Lee DH, Yoo JH, Cho JY, Hahm KB, Bang CS, Baik GH, Shin IS, Kim JB, Suk KT, Yoon JH, Kim YS, Kim DJ * Helicobacter pylori Eradication for Prevention of Metachronous Recurrence after Endoscopic Resection of Early Gastric Cancer(667 views) N Engl J Med (ISSN: 0028-4793, 0028-4793linking, 1533-4406electronic), 2015 Jun; 30642104201566393291: 749-756. Impact Factor:59.558 ViewExport to BibTeXExport to EndNote