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Publikationer i urvalet

17 träffar

Bibliografisk träff 2022-11-29

Rational design, synthesis, and pharmacological evaluation of a cohort of novel beta-adrenergic receptors ligands enables an assessment of structure-activity relationships.

Tricomi J, Landini L, Nieddu V, Cavallaro U, Baker JG, Papakyriakou A, Richichi B.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114961

Bibliografisk träff 2021-02-23

A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models.

Singh SS, Mattheolabakis G, Gu X, Withers S, Dahal A, Jois S.

Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2021.113312

Bibliografisk träff 2017-09-12

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation.

Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, Fish PV, Igoe NM, Bayle ED, Haendler B, Oppermann UCT, Buffa F, Brennan PE, Müller S, Gingras AC, Odgren PR, Birnbaum MJ, Knapp S.

ACS Chem Biol · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acschembio.7b00481

Bibliografisk träff 2016-03-03

Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.

Waszkielewicz AM, Gunia-Krzyżak A, Powroźnik B, Słoczyńska K, Pękala E, Walczak M, Bednarski M, Żesławska E, Nitek W, Marona H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2016.03.006

Bibliografisk träff 2015-01-03

Insights on the role of boron containing moieties in the design of new potent and efficient agonists targeting the β2 adrenoceptor.

Soriano-Ursúa MA, Arias-Montaño JA, Correa-Basurto J, Hernández-Martínez CF, López-Cabrera Y, Castillo-Hernández MC, Padilla-Martínez II, Trujillo-Ferrara JG.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2014.12.077

Bibliografisk träff 2013-05-10

Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.

Mistry SN, Baker JG, Fischer PM, Hill SJ, Gardiner SM, Kellam B.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm400348g

Bibliografisk träff 2013-03-24

Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.

Veinberg G, Vorona M, Zvejniece L, Vilskersts R, Vavers E, Liepinsh E, Kazoka H, Belyakov S, Mishnev A, Kuznecovs J, Vikainis S, Orlova N, Lebedev A, Ponomaryov Y, Dambrova M.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2013.03.016

Bibliografisk träff 2013-02-08

Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.

Cappelli A, Manini M, Valenti S, Castriconi F, Giuliani G, Anzini M, Brogi S, Butini S, Gemma S, Campiani G, Giorgi G, Mennuni L, Lanza M, Giordani A, Caselli G, Letari O, Makovec F.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2013.01.044

Bibliografisk träff 2011-07-18

Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.

Dolusić E, Larrieu P, Moineaux L, Stroobant V, Pilotte L, Colau D, Pochet L, Van den Eynde B, Masereel B, Wouters J, Frédérick R.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm2006782

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 2009-03-01

Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.

Kern C, Meyer T, Droux S, Schollmeyer D, Miculka C.

J Med Chem · journal article · DOI 10.1021/jm801211c

Bibliografisk träff 2008-12-25

Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist.

Soriano-Ursúa MA, Valencia-Hernández I, Arellano-Mendoza MG, Correa-Basurto J, Trujillo-Ferrara JG.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2008.12.016

Bibliografisk träff 2008-11-01

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.

Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR, Strakhova MI, Vortherms TA, Wakefield BD, Wetter JM, Witte DG, Honore P, Esbenshade TA, Brioni JD, Cowart MD.

J Med Chem · journal article · DOI 10.1021/jm8007618

Bibliografisk träff 2006-06-25

Coupling ligand structure to specific conformational switches in the beta2-adrenoceptor.

Yao X, Parnot C, Deupi X, Ratnala VR, Swaminath G, Farrens D, Kobilka B.

Nat Chem Biol · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1038/nchembio801

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 1988-11-01

Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.

el Tayar N, Carrupt PA, Van de Waterbeemd H, Testa B.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/jm00119a004

Bibliografisk träff 1985-03-01

[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.

McNeal ET, Lewandowski GA, Daly JW, Creveling CR.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm00381a019