Design, synthesis and evaluation of polar head group containing 2-keto-oxazole inhibitors of FAAH.
Rusch M, Zahov S, Vetter IR, Lehr M, Hedberg C.
Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2011.11.027 PUBLIKATIONSREGISTRET
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50 träffarSAR and LC/MS studies of β-lactamic inhibitors of human fatty acid amide hydrolase (hFAAH): evidence of a nonhydrolytic process.
Feledziak M, Muccioli GG, Lambert DM, Marchand-Brynaert J.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm200723mBiphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability.
Vacondio F, Silva C, Lodola A, Carmi C, Rivara S, Duranti A, Tontini A, Sanchini S, Clapper JR, Piomelli D, Tarzia G, Mor M.
Eur J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.ejmech.2011.07.021The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).
Otrubova K, Ezzili C, Boger DL.
Bioorg Med Chem Lett · research-article; review; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2011.06.096New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis.
Andrzejak V, Muccioli GG, Body-Malapel M, El Bakali J, Djouina M, Renault N, Chavatte P, Desreumaux P, Lambert DM, Millet R.
Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2011.04.057Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain.
Ahn K, Smith SE, Liimatta MB, Beidler D, Sadagopan N, Dudley DT, Young T, Wren P, Zhang Y, Swaney S, Van Becelaere K, Blankman JL, Nomura DK, Bhattachar SN, Stiff C, Nomanbhoy TK, Weerapana E, Johnson DS, Cravatt BF.
J Pharmacol Exp Ther · comparative study; research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1124/jpet.111.180257Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2011.02.052Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.
Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, Ahn K.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml100190tTransient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Baraldi PG, Preti D, Materazzi S, Geppetti P.
J Med Chem · review; journal article · DOI 10.1021/jm100062hSynthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors.
Onnis V, Congiu C, Björklund E, Hempel F, Söderström E, Fowler CJ.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm901891p1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A(2)alpha and fatty acid amide hydrolase.
Forster L, Ludwig J, Kaptur M, Bovens S, Elfringhoff AS, Holtfrerich A, Lehr M.
Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2009.11.028Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.
Hart T, Macias AT, Benwell K, Brooks T, D'Alessandro J, Dokurno P, Francis G, Gibbons B, Haymes T, Kennett G, Lightowler S, Mansell H, Matassova N, Misra A, Padfield A, Parsons R, Pratt R, Robertson A, Walls S, Wong M, Roughley S.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2009.05.097Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH).
Johnson DS, Ahn K, Kesten S, Lazerwith SE, Song Y, Morris M, Fay L, Gregory T, Stiff C, Dunbar JB, Liimatta M, Beidler D, Smith S, Nomanbhoy TK, Cravatt BF.
Bioorg Med Chem Lett · research-article; journal article · DOI 10.1016/j.bmcl.2009.03.080The synthesis and biological evaluation of para-substituted phenolic N-alkyl carbamates as endocannabinoid hydrolyzing enzyme inhibitors.
Minkkilä A, Myllymäki MJ, Saario SM, Castillo-Melendez JA, Koskinen AM, Fowler CJ, Leppänen J, Nevalainen T.
Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2009.01.007Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors.
Wang X, Sarris K, Kage K, Zhang D, Brown SP, Kolasa T, Surowy C, El Kouhen OF, Muchmore SW, Brioni JD, Stewart AO.
J Med Chem · journal article · DOI 10.1021/jm801042aDiscovery and development of fatty acid amide hydrolase (FAAH) inhibitors.
Seierstad M, Breitenbucher JG.
J Med Chem · review; journal article · DOI 10.1021/jm800311kThiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Keith JM, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, Webb M, Karbarz MJ, Brown S, Wilson S, Scott B, Tham CS, Luo L, Palmer J, Wennerholm M, Chaplan S, Breitenbucher JG.
Bioorg Med Chem Lett · comparative study; journal article · DOI 10.1016/j.bmcl.2008.07.081Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.
Mor M, Lodola A, Rivara S, Vacondio F, Duranti A, Tontini A, Sanchini S, Piersanti G, Clapper JR, King AR, Tarzia G, Piomelli D.
J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm701631zFatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system.
Saario SM, Poso A, Juvonen RO, Järvinen T, Salo-Ahen OM.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm060394qCyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.
Mor M, Rivara S, Lodola A, Plazzi PV, Tarzia G, Duranti A, Tontini A, Piersanti G, Kathuria S, Piomelli D.
J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm031140x