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Publikationer i urvalet

26 träffar

Bibliografisk träff 2019-05-29

Computer-Aided Selective Optimization of Side Activities of Talinolol.

Hiesinger K, Kramer JS, Achenbach J, Moser D, Weber J, Wittmann SK, Morisseau C, Angioni C, Geisslinger G, Kahnt AS, Kaiser A, Proschak A, Steinhilber D, Pogoryelov D, Wagner K, Hammock BD, Proschak E.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.9b00075

Bibliografisk träff 2018-08-18

An antimycobacterial pleuromutilin analogue effective against dormant bacilli.

Lemieux MR, Siricilla S, Mitachi K, Eslamimehr S, Wang Y, Yang D, Pressly JD, Kong Y, Park F, Franzblau SG, Kurosu M.

Bioorg Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2018.07.034

Bibliografisk träff 2018-07-27

Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo.

Vesci L, Milazzo FM, Stasi MA, Pace S, Manera F, Tallarico C, Cini E, Petricci E, Manetti F, De Santis R, Giannini G.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.07.053

Bibliografisk träff 2017-11-01

Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker.

Do HT, Wang HY, Li H, Chreifi G, Poulos TL, Silverman RB.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.7b01356

Bibliografisk träff 2017-09-28

The antitubercular activity of various nitro(triazole/imidazole)-based compounds.

Papadopoulou MV, Bloomer WD, Rosenzweig HS.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2017.09.037

Bibliografisk träff 2017-08-18

Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.

Qi Q, Obianyo O, Du Y, Fu H, Li S, Ye K.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.7b00228

Bibliografisk träff 2017-08-04

Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.

Pensa AV, Cinelli MA, Li H, Chreifi G, Mukherjee P, Roman LJ, Martásek P, Poulos TL, Silverman RB.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.7b00835

Bibliografisk träff 2017-04-19

Nitrile in the Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors.

Cinelli MA, Li H, Chreifi G, Poulos TL, Silverman RB.

J Med Chem · research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.7b00259

Bibliografisk träff 2017-02-21

Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.

Eissa IH, Mohammad H, Qassem OA, Younis W, Abdelghany TM, Elshafeey A, Abd Rabo Moustafa MM, Seleem MN, Mayhoub AS.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.02.044

Bibliografisk träff 2016-04-22

Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.

Bassetto M, Ferla S, Pertusati F, Kandil S, Westwell AD, Brancale A, McGuigan C.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2016.04.052

Bibliografisk träff 2015-10-27

Phenyl Ether- and Aniline-Containing 2-Aminoquinolines as Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase.

Cinelli MA, Li H, Pensa AV, Kang S, Roman LJ, Martásek P, Poulos TL, Silverman RB.

J Med Chem · research-article; journal article · DOI 10.1021/acs.jmedchem.5b01330

Bibliografisk träff 2015-09-04

3-Nitrotriazole-based piperazides as potent antitrypanosomal agents.

Papadopoulou MV, Bloomer WD, Rosenzweig HS, O'Shea IP, Wilkinson SR, Kaiser M.

Eur J Med Chem · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1016/j.ejmech.2015.08.042

Bibliografisk träff 2015-08-24

Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.

Papadopoulou MV, Bloomer WD, Rosenzweig HS, O'Shea IP, Wilkinson SR, Kaiser M, Chatelain E, Ioset JR.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2015.08.014

Bibliografisk träff 2015-06-16

Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.

Davis DC, Mohammad H, Kyei-Baffour K, Younis W, Creemer CN, Seleem MN, Dai M.

Eur J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.ejmech.2015.06.031

Bibliografisk träff 2014-12-29

Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.

Mukherjee P, Li H, Sevrioukova I, Chreifi G, Martásek P, Roman LJ, Poulos TL, Silverman RB.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm501719e

Bibliografisk träff 2014-03-20

A high-throughput cell-based method to predict the unbound drug fraction in the brain.

Mateus A, Matsson P, Artursson P.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm401963n

Bibliografisk träff 2014-02-10

Simplified 2-aminoquinoline-based scaffold for potent and selective neuronal nitric oxide synthase inhibition.

Cinelli MA, Li H, Chreifi G, Martásek P, Roman LJ, Poulos TL, Silverman RB.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm401838x

Bibliografisk träff 2011-11-17

Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.

Farrell TL, Poquet L, Dew TP, Barber S, Williamson G.

Drug Metab Dispos · research support, non-u.s. gov't; validation study; journal article · DOI 10.1124/dmd.111.041665

Bibliografisk träff 2011-04-07

Species independence in brain tissue binding using brain homogenates.

Di L, Umland JP, Chang G, Huang Y, Lin Z, Scott DO, Troutman MD, Liston TE.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.111.038778

Bibliografisk träff 2010-02-01

Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.

Varma MV, Obach RS, Rotter C, Miller HR, Chang G, Steyn SJ, El-Kattan A, Troutman MD.

J Med Chem · journal article · DOI 10.1021/jm901371v

Bibliografisk träff 2009-08-01

Physicochemical determinants of human renal clearance.

Varma MV, Feng B, Obach RS, Troutman MD, Chupka J, Miller HR, El-Kattan A.

J Med Chem · journal article · DOI 10.1021/jm900403j

Bibliografisk träff 2008-04-21

Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.

Obach RS, Lombardo F, Waters NJ.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.108.020479

Bibliografisk träff 2004-05-01

Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo.

Collett A, Tanianis-Hughes J, Hallifax D, Warhurst G.

Pharm Res · journal article · DOI 10.1023/b:pham.0000026434.82855.69

Bibliografisk träff 2003-08-01

pH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: implications for drug-drug interactions.

Neuhoff S, Ungell AL, Zamora I, Artursson P.

Pharm Res · research support, non-u.s. gov't; journal article · DOI 10.1023/a:1025032511040

Bibliografisk träff 2003-08-01

Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.

Troutman MD, Thakker DR.

Pharm Res · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1023/a:1025001131513

Bibliografisk träff 1999-01-01

Characterization of binding properties to human P-glycoprotein: development of a [3H]verapamil radioligand-binding assay.

Döppenschmitt S, Langguth P, Regårdh CG, Andersson TB, Hilgendorf C, Spahn-Langguth H.

J Pharmacol Exp Ther · research support, non-u.s. gov't; journal article · DOI 10.1016/s0022-3565(24)37960-1