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Volume 48; Issue 1

Journal of Medicinal Chemistry

Volume 48; Issue 1

1

Interaction Profiles of Protein Kinase−Inhibitor Complexes and Their Application to Virtual Screening

Chuaqui, Claudio, Deng, Zhan, Singh, Juswinder

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 868 KB

english, 2005

2

Acid−Base Profiling of Imatinib (Gleevec) and Its Fragments

Szakács, Zoltán, Béni, Szabolcs, Varga, Zoltán, Örfi, László, Kéri, György, Noszál, Béla

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 255 KB

english, 2005

3

5-Substituted, 6-Substituted, and Unsubstituted 3-Heteroaromatic Pyridine Analogues of Nicotine as Selective Inhibitors of Cytochrome P-450 2A6

Denton, Travis T., Zhang, Xiaodong, Cashman, John R.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 239 KB

english, 2005

4

Optimization in Drug Discovery. In Vitro Methods Edited by Zhengyin Yan and Gary W. Caldwell. Humana Press, Totowa, NJ. 2004. xv + 418 pp. 16 × 23.5 cm. ISBN 1-588-29-332-7. $135.00.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 31 KB

english, 2005

5

Propidium-Based Polyamine Ligands as Potent Inhibitors of Acetylcholinesterase and Acetylcholinesterase-Induced Amyloid-β Aggregation

Bolognesi, Maria Laura, Andrisano, Vincenza, Bartolini, Manuela, Banzi, Rita, Melchiorre, Carlo

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 151 KB

english, 2005

6

Synthesis and Structure−Activity Relationships of 1-Aralkyl-4-Benzylpiperidine and 1-Aralkyl-4-Benzylpiperazine Derivatives as Potent σ Ligands

Costantino, Luca, Gandolfi, Francesca, Sorbi, Claudia, Franchini, Silvia, Prezzavento, Orazio, Vittorio, Franco, Ronsisvalle, Giuseppe, Leonardi, Amedeo, Poggesi, Elena, Brasili, Livio

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 272 KB

english, 2005

7

Docking and 3-D QSAR Studies on Indolyl Aryl Sulfones. Binding Mode Exploration at the HIV-1 Reverse Transcriptase Non-Nucleoside Binding Site and Design of Highly Active N-(2-Hydroxyethyl)carboxamide and N-(2-Hydroxyethyl)carbohydrazide Derivatives

Artico, Marino, Ragno, Rino, De Martino, Gabriella, La Regina, Giuseppe, Coluccia, Antonio, Di Pasquali, Alessandra, Silvestri, Romano

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 549 KB

english, 2005

8

(2 R )-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3- a ]pyrazin- 7(8 H )-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Kim, Dooseop, Wang, Liping, Beconi, Maria, Eiermann, George J., Fisher, Michael H., He, Huaibing, Hickey, Gerard J., Kowalchick, Jennifer E., Leiting, Barbara, Lyons, Kathryn, Marsilio, Frank, McCann,

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 327 KB

english, 2005

9

Discovery of Potent, Orally Available Vanilloid Receptor-1 Antagonists. Structure−Activity Relationship of N -Aryl Cinnamides

Doherty, Elizabeth M., Fotsch, Christopher, Bo, Yunxin, Chakrabarti, Partha P., Chen, Ning, Gavva, Narender, Han, Nianhe, Kelly, Michael G., Kincaid, John, Klionsky, Lana, Liu, Qingyian, Ognyanov, Vas

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 321 KB

english, 2005

10

β-Diketo Acid Pharmacophore Hypothesis. 1. Discovery of a Novel Class of HIV-1 Integrase Inhibitors

Dayam, Raveendra, Sanchez, Tino, Clement, Omoshile, Shoemaker, Robert, Sei, Shizuko, Neamati, Nouri

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 608 KB

english, 2005

11

Dual Angiotensin II and Endothelin A Receptor Antagonists: Synthesis of 2‘-Substituted N-3-Isoxazolyl Biphenylsulfonamides with Improved Potency and Pharmacokinetics

Murugesan, Natesan, Gu, Zhengxiang, Fadnis, Leena, Tellew, John E., Baska, Rose Ann F., Yang, Yifan, Beyer, Sophie M., Monshizadegan, Hossain, Dickinson, Kenneth E., Valentine, Maria T., Humphreys, W.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 266 KB

english, 2005

12

Modeled Structure of a G-Protein-Coupled Receptor: The Cholecystokinin-1 Receptor

Archer-Lahlou, Elodie, Tikhonova, Irina, Escrieut, Chantal, Dufresne, Marlène, Seva, Catherine, Pradayrol, Lucien, Moroder, Luis, Maigret, Bernard, Fourmy, Daniel

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 425 KB

english, 2005

13

HIV-Reverse Transcriptase Inhibition: Inclusion of Ligand-Induced Fit by Cross-Docking Studies

Ragno, Rino, Frasca, Simona, Manetti, Fabrizio, Brizzi, Antonella, Massa, Silvio

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 1.04 MB

english, 2005

14

Combined Target-Based and Ligand-Based Drug Design Approach as a Tool To Define a Novel 3D-Pharmacophore Model of Human A 3 Adenosine Receptor Antagonists: Pyrazolo[4,3- e ]1,2,4-triazolo[1,5- c ]pyrimidine Derivatives as a Key Study

Moro, Stefano, Braiuca, Paolo, Deflorian, Francesca, Ferrari, Cristina, Pastorin, Giorgia, Cacciari, Barbara, Baraldi, Pier Giovanni, Varani, Katia, Borea, Pier Andrea, Spalluto, Giampiero

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 294 KB

english, 2005

15

Synthesis and Biological Properties of New Stilbene Derivatives of Resveratrol as New Selective Aryl Hydrocarbon Modulators

de Medina, Philippe, Casper, Robert, Savouret, Jean-François, Poirot, Marc

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 90 KB

english, 2005

16

Retro Hydrazino-azapeptoids as Peptidomimetics of Proteasome Inhibitors

Aubin, Sandrine, Martin, Bénédicte, Delcros, Jean-Guy, Arlot-Bonnemains, Yannick, Baudy-Floc'h, Michèle

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 141 KB

english, 2005

17

Control of Hepatitis C: A Medicinal Chemistry Perspective

Gordon, Christopher P., Keller, Paul A.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 650 KB

english, 2005

18

Derivation and Validation of Toxicophores for Mutagenicity Prediction

Kazius, Jeroen, McGuire, Ross, Bursi, Roberta

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 175 KB

english, 2005

19

Inhibition of Nucleoside Transport Proteins by C 8 -Alkylamine-Substituted Purines

Tromp, Reynier A., Spanjersberg, Ronald F., von Frijtag Drabbe Künzel, Jacobien K., IJzerman, Adriaan P.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 173 KB

english, 2005

20

4-Hydroxymethyl-1,6,8-trimethylfuro[2,3- h ]quinolin-2(1 H )-one Induces Mitochondrial Dysfunction and Apoptosis upon Its Intracellular Oxidation

Chilin, Adriana, Dodoni, Giuliano, Frezza, Christian, Guiotto, Adriano, Barbieri, Vera, Di Lisa, Fabio, Canton, Marcella

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 413 KB

english, 2005

21

3-Hydroxymethyl-7-( N -substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline Inhibitors of Phenylethanolamine N -Methyltransferase that Display Remarkable Potency and Selectivity 1

Grunewald, Gary L., Romero, F. Anthony, Criscione, Kevin R.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 233 KB

english, 2005

22

Structure−Activity Relationships and Effects on Neuroactive Steroid Synthesis in a Series of 2-Phenylimidazo[1,2- a ]pyridineacetamide Peripheral Benzodiazepine Receptors Ligands

Trapani, Giuseppe, Laquintana, Valentino, Denora, Nunzio, Trapani, Adriana, Lopedota, Angela, Latrofa, Andrea, Franco, Massimo, Serra, Mariangela, Pisu, Maria Giuseppina, Floris, Ivan, Sanna, Enrico,

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 222 KB

english, 2005

23

In Vitro and in Vivo Anti-Leishmanial Activity of Triterpenoid Saponins Isolated from Maesa b alansae and Some Chemical Derivatives

Germonprez, Nils, Maes, Louis, Van Puyvelde, Luc, Van Tri, Mai, Tuan, Duong Anh, De Kimpe, Norbert

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 125 KB

english, 2005

24

4-(2-[2-(2( R )-Methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and Related 2-Aminoethylbenzofuran H 3 Receptor Antagonists Potently Enhance Cognition and Attention

Cowart, Marlon, Faghih, Ramin, Curtis, Michael P., Gfesser, Gregory A., Bennani, Youssef L., Black, Lawrence A., Pan, Liping, Marsh, Kennan C., Sullivan, James P., Esbenshade, Timothy A., Fox, Gerard

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 371 KB

english, 2005

25

2-(4-Alkylpiperazin-1-yl)quinolines as a New Class of Imidazole-Free Histamine H 3 Receptor Antagonists

Zaragoza, Florencio, Stephensen, Henrik, Peschke, Bernd, Rimvall, Karin

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 130 KB

english, 2005

26

Design and Crystal Structures of Protein Kinase B-Selective Inhibitors in Complex with Protein Kinase A and Mutants

Breitenlechner, Christine B., Friebe, Walter-Gunar, Brunet, Emmanuel, Werner, Guido, Graul, Klaus, Thomas, Ulrike, Künkele, Klaus-Peter, Schäfer, Wolfgang, Gassel, Michael, Bossemeyer, Dirk, Huber, Ro

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 916 KB

english, 2005

27

Crystal Structures of Staphylococcus aureus Methionine Aminopeptidase Complexed with Keto Heterocycle and Aminoketone Inhibitors Reveal the Formation of a Tetrahedral Intermediate.

Douangamath, Alice, Dale, Glenn E., D'Arcy, Allan, Almstetter, Michael, Eckl, Robert, Frutos-Hoener, Annabelle, Henkel, Bernd, Illgen, Katrin, Nerdinger, Sven, Schulz, Henk, Mac Sweeney, Aengus, Thorm

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 38 KB

english, 2005

28

Discovery of Corticotropin Releasing Factor 2 Receptor Selective Sauvagine Analogues for Treatment of Skeletal Muscle Atrophy

Isfort, Robert J., Wang, Feng, Tscheiner, Michelle, Donnelly, Elizabeth, Bauer, Mary Beth, Lefever, Frank, Hinkle, Richard T., Mazur, Adam W.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 53 KB

english, 2005

29

β-Glucuronidase-Cleavable Prodrugs of O 6 -Benzylguanine and O 6 -Benzyl-2‘-deoxyguanosine

Wei, Guangping, Loktionova, Natalia A., Pegg, Anthony E., Moschel, Robert C.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 129 KB

english, 2005

30

Hit-Directed Nearest-Neighbor Searching

Shanmugasundaram, Veerabahu, Maggiora, Gerald M., Lajiness, Michael S.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 280 KB

english, 2005

31

Synthesis and Ligand Binding of Tropane Ring Analogues of Paroxetine

Keverline-Frantz, Kathryn I., Boja, John W., Kuhar, Michael J., Abraham, Philip, Burgess, Jason P., Lewin, Anita H., Carroll, F. Ivy

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 38 KB

english, 2005

32

The Effects of Conformational Constraints and Steric Bulk in the Amino Acid Moiety of Philanthotoxins on AMPAR Antagonism

Jørgensen, Malene R., Olsen, Christian A., Mellor, Ian R., Usherwood, Peter N. R., Witt, Matthias, Franzyk, Henrik, Jaroszewski, Jerzy W.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 293 KB

english, 2005

33

Potent Bombesin-like Peptides for GRP-Receptor Targeting of Tumors with 99m Tc: A Preclinical Study

Nock, Berthold A., Nikolopoulou, Anastasia, Galanis, Athanassios, Cordopatis, Paul, Waser, Beatrice, Reubi, Jean-Claude, Maina, Theodosia

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 452 KB

english, 2005

34

Design, Synthesis, and Biological Evaluation of Prazosin-Related Derivatives as Multipotent Compounds

Antonello, Alessandra, Hrelia, Patrizia, Leonardi, Amedeo, Marucci, Gabriella, Rosini, Michela, Tarozzi, Andrea, Tumiatti, Vincenzo, Melchiorre, Carlo

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 72 KB

english, 2005

35

Design and NMR Characterization of Active Analogues of Compstatin Containing Non-Natural Amino Acids

Mallik, Buddhadeb, Katragadda, Madan, Spruce, Lynn A., Carafides, Caterina, Tsokos, Christos G., Morikis, Dimitrios, Lambris, John D.

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 580 KB

english, 2005

36

Nucleotides and Pronucleotides of 2,2-Bis(hydroxymethyl)methylenecyclopropane Analogues of Purine Nucleosides: Synthesis and Antiviral Activity

Yan, Zhaohua, Kern, Earl R., Gullen, Elizabeth, Cheng, Yung-Chi, Drach, John C., Zemlicka, Jiri

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 204 KB

english, 2005

37

Phenazine 5,10-Dioxide Derivatives as Hypoxic Selective Cytotoxins

Cerecetto, Hugo, GonzÃ¡lez, Mercedes, Lavaggi, Ma Laura, Azqueta, Amaia, LÃ³pez de Cerain, Adela, Monge, Antonio

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 63 KB

english, 2005

38

10.1021/jm040198o

Journal:

Journal of Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 31 KB

english, 2005