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Publikationer i urvalet

17 träffar

Bibliografisk träff 2010-07-21

Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relationships.

Hayashi S, Nakata E, Morita A, Mizuno K, Yamamura K, Kato A, Ohashi K.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2010.07.034

Bibliografisk träff 2008-06-25

In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.

Plouffe D, Brinker A, McNamara C, Henson K, Kato N, Kuhen K, Nagle A, Adrián F, Matzen JT, Anderson P, Nam TG, Gray NS, Chatterjee A, Janes J, Yan SF, Trager R, Caldwell JS, Schultz PG, Zhou Y, Winzeler EA.

Proc Natl Acad Sci U S A · research support, non-u.s. gov't; research-article; journal article · DOI 10.1073/pnas.0802982105

Bibliografisk träff 2005-11-01

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.

Minetti P, Tinti MO, Carminati P, Castorina M, Di Cesare MA, Di Serio S, Gallo G, Ghirardi O, Giorgi F, Giorgi L, Piersanti G, Bartoccini F, Tarzia G.

J Med Chem · journal article · DOI 10.1021/jm058018d

Bibliografisk träff 2005-08-01

Development of a three-dimensional model for the N-methyl-D-aspartate NR2A subunit.

Grazioso G, Moretti L, Scapozza L, De Amici M, De Micheli C.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm050174x

Bibliografisk träff 2002-09-01

Multisubstrate analogue inhibitors of glucosamine-6-phosphate synthase from Candida albicans.

Chittur S, Griffith R.

Bioorg Med Chem Lett · research support, u.s. gov't, p.h.s.; journal article · DOI 10.1016/s0960-894x(02)00510-3

Bibliografisk träff 2001-05-01

Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.

Baudy RB, Fletcher H, Yardley JP, Zaleska MM, Bramlett DR, Tasse RP, Kowal DM, Katz AH, Moyer JA, Abou-Gharbia M.

J Med Chem · journal article · DOI 10.1021/jm000385w

Bibliografisk träff 1998-01-01

Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid (EAA-090), a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere.

Kinney WA, Abou-Gharbia M, Garrison DT, Schmid J, Kowal DM, Bramlett DR, Miller TL, Tasse RP, Zaleska MM, Moyer JA.

J Med Chem · journal article · DOI 10.1021/jm970504g

Bibliografisk träff 1993-02-01

Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.

Baudy RB, Greenblatt LP, Jirkovsky IL, Conklin M, Russo RJ, Bramlett DR, Emrey TA, Simmonds JT, Kowal DM, Stein RP.

J Med Chem · journal article · DOI 10.1021/jm00055a004

Bibliografisk träff 1992-09-01

6-substituted decahydroisoquinoline-3-carboxylic acids as potent and selective conformationally constrained NMDA receptor antagonists.

Ornstein PL, Schoepp DD, Arnold MB, Augenstein NK, Lodge D, Millar JD, Chambers J, Campbell J, Paschal JW, Zimmerman DM.

J Med Chem · journal article · DOI 10.1021/jm00097a012

Bibliografisk träff 1992-05-01

Modeling of competitive phosphono amino acid NMDA receptor antagonists.

Whitten JP, Harrison BL, Weintraub HJ, McDonald IA.

J Med Chem · journal article · DOI 10.1021/jm00087a002

Bibliografisk träff 1992-04-01

Generation of N-methyl-D-aspartate agonist and competitive antagonist pharmacophore models. Design and synthesis of phosphonoalkyl-substituted tetrahydroisoquinolines as novel antagonists.

Ortwine DF, Malone TC, Bigge CF, Drummond JT, Humblet C, Johnson G, Pinter GW.

J Med Chem · comparative study; journal article · DOI 10.1021/jm00086a004

Bibliografisk träff 1991-01-01

Synthesis and biological evaluation of cyclopropyl analogues of 2-amino-5-phosphonopentanoic acid.

Dappen MS, Pellicciari R, Natalini B, Monahan JB, Chiorri C, Cordi AA.

J Med Chem · comparative study; journal article · DOI 10.1021/jm00105a024

Bibliografisk träff 1991-01-01

4-(Tetrazolylalkyl)piperidine-2-carboxylic acids. Potent and selective N-methyl-D-aspartic acid receptor antagonists with a short duration of action.

Ornstein PL, Schoepp DD, Arnold MB, Leander JD, Lodge D, Paschal JW, Elzey T.

J Med Chem · comparative study; journal article · DOI 10.1021/jm00105a016

Bibliografisk träff 1990-11-01

(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.

Whitten JP, Baron BM, Muench D, Miller F, White HS, McDonald IA.

J Med Chem · journal article · DOI 10.1021/jm00173a009

Bibliografisk träff 1990-10-01

New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.

Hays SJ, Bigge CF, Novak PM, Drummond JT, Bobovski TP, Rice MJ, Johnson G, Brahce LJ, Coughenour LL.

J Med Chem · journal article · DOI 10.1021/jm00172a037

Bibliografisk träff 1989-09-01

4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.

Hutchison AJ, Williams M, Angst C, de Jesus R, Blanchard L, Jackson RH, Wilusz EJ, Murphy DE, Bernard PS, Schneider J.

J Med Chem · journal article · DOI 10.1021/jm00129a025

Bibliografisk träff 1989-04-01

Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists.

Ornstein PL, Schaus JM, Chambers JW, Huser DL, Leander JD, Wong DT, Paschal JW, Jones ND, Deeter JB.

J Med Chem · comparative study; journal article · DOI 10.1021/jm00124a015