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Volume 47; Issue 10

Journal of Medicinal Chemistry

Volume 47; Issue 10

1

Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability: Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α-Aminoacyl-l-cis-4,5-methanoprolinenitrile-Based Inhibitors

Magnin, David R., Robl, Jeffrey A., Sulsky, Richard B., Augeri, David J., Huang, Yanting, Simpkins, Ligaya M., Taunk, Prakash C., Betebenner, David A., Robertson, James G., Abboa-Offei, Benoni E.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 199 KB

english, 2004

2

Discovery of Diarylacrylonitriles as a Novel Series of Small Molecule Sortase A Inhibitors

Oh, Ki-Bong, Kim, Soo-Hwan, Lee, Jaekwang, Cho, Won-Jea, Lee, Taeho, Kim, Sanghee

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 156 KB

english, 2004

3

New 1,4-Dihydropyridines Endowed with NO-Donor and Calcium Channel Agonist Properties

Visentin, Sonja, Rolando, Barbara, Di Stilo, Antonella, Fruttero, Roberta, Novara, Monica, Carbone, Emilio, Roussel, Christian, Vanthuyne, Nicolas, Gasco, Alberto

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 111 KB

english, 2004

4

Cytotoxic α-Halogenoacrylic Derivatives of Distamycin A and Congeners

Beria, Italo, Baraldi, Pier Giovanni, Cozzi, Paolo, Caldarelli, Marina, Geroni, Cristina, Marchini, Sergio, Mongelli, Nicola, Romagnoli, Romeo

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 388 KB

english, 2004

5

Design, Synthesis, Structural Studies, Biological Evaluation, and Computational Simulations of Novel Potent AT1 Angiotensin II Receptor Antagonists Based on the 4-Phenylquinoline Structure

Cappelli, Andrea, Pericot Mohr, Gal.la, Gallelli, Andrea, Rizzo, Milena, Anzini, Maurizio, Vomero, Salvatore, Mennuni, Laura, Ferrari, Flora, Makovec, Francesco, Menziani, M. Cristina

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 673 KB

english, 2004

6

Conformational Analysis of Drug-Like Molecules Bound to Proteins: An Extensive Study of Ligand Reorganization upon Binding

Perola, Emanuele, Charifson, Paul S.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 166 KB

english, 2004

7

Oral Bioavailability of a New Class of μ-Opioid Receptor Agonists Containing 3,6-Bis[Dmt-NH(CH2)n]-2(1H)-pyrazinone with Central-Mediated Analgesia

Jinsmaa, Yunden, Miyazaki, Anna, Fujita, Yoshio, Li, Tingyou, Fujisawa, Yutaka, Shiotani, Kimitaka, Tsuda, Yuko, Yokoi, Toshio, Ambo, Akihiro, Sasaki, Yusuke

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 268 KB

english, 2004

8

Roles of Conformational and Positional Adaptability in Structure-Based Design of TMC125-R165335 (Etravirine) and Related Non-nucleoside Reverse Transcriptase Inhibitors That Are Highly Potent and Effective against Wild-Type and Drug-Resistant HIV-1 Variants

Das, Kalyan, Clark,, Arthur D., Lewi, Paul J., Heeres, Jan, de Jonge, Marc R., Koymans, Lucien M. H., Vinkers, H. Maarten, Daeyaert, Frederik, Ludovici, Donald W., Kukla, Michael J.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 694 KB

english, 2004

9

Development of Irreversible Diphenyl Phosphonate Inhibitors for Urokinase Plasminogen Activator

Joossens, J., Van der Veken, P., Lambeir, A.-M., Augustyns, K., Haemers, A.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 63 KB

english, 2004

10

Rational Design and Synthesis of Novel Dimeric Diketoacid-Containing Inhibitors of HIV-1 Integrase: Implication for Binding to Two Metal Ions on the Active Site of Integrase

Long, Ya-Qiu, Jiang, Xiao-Hua, Dayam, Raveendra, Sanchez, Tino, Shoemaker, Robert, Sei, Shizuko, Neamati, Nouri

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 845 KB

english, 2004

11

General Model for Estimation of the Inhibition of Protein Kinases Using Monte Carlo Simulations

Tominaga, Yukio, Jorgensen, William L.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 538 KB

english, 2004

12

New Arylpiperazine 5-HT 1A Receptor Ligands Containing the Pyrimido[2,1- f ]purine Fragment: Synthesis, in Vitro, and in Vivo Pharmacological Evaluation

Jurczyk, Sławomir, Kołaczkowski, Marcin, Maryniak, Ewa, Zajdel, Paweł, Pawłowski, Maciej, Tatarczyńska, Ewa, Kłodzińska, Aleksandra, Chojnacka-Wójcik, Ewa, Bojarski, Andrzej J., Charakchieva-Minol, Si

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 98 KB

english, 2004

13

Discovery of Embelin as a Cell-Permeable, Small-Molecular Weight Inhibitor of XIAP through Structure-Based Computational Screening of a Traditional Herbal Medicine Three-Dimensional Structure Database

Nikolovska-Coleska, Zaneta, Xu, Liang, Hu, Zengjian, Tomita, York, Li, Peng, Roller, Peter P., Wang, Renxiao, Fang, Xueliang, Guo, Ribo, Zhang, Manchao, Lippman, Marc E., Yang, Dajun, Wang, Shaomeng

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 438 KB

english, 2004

14

Peptide-Based Inhibitors of the Hepatitis C Virus NS3 Protease: Structure−Activity Relationship at the C -Terminal Position

Rancourt, Jean, Cameron, Dale R., Gorys, Vida, Lamarre, Daniel, Poirier, Martin, Thibeault, Diane, Llinàs-Brunet, Montse

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 267 KB

english, 2004

15

Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-{2-methoxy-1( R )-4-(trifluoromethyl)phenyl}ethyl-3( S )-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist

Tagat, Jayaram R., McCombie, Stuart W., Nazareno, Dennis, Labroli, Marc A., Xiao, Yushi, Steensma, Ruo W., Strizki, Julie M., Baroudy, Bahige M., Cox, Kathleen, Lachowicz, Jean, Varty, Geoffrey, Watki

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 78 KB

english, 2004

16

Inhibitors of Serine Proteases as Potential Therapeutic Agents: The Road from Thrombin to Tryptase to Cathepsin G.

Maryanoff, Bruce E.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 10 KB

english, 2004

17

Lessons Learned from Marketed and Investigational Prodrugs

Ettmayer, Peter, Amidon, Gordon L., Clement, Bernd, Testa, Bernard

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 231 KB

english, 2004

18

Identification of 4-(1 H -Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H 3 Receptor Agonist

Kitbunnadaj, Ruengwit, Zuiderveld, Obbe P., Christophe, Bernard, Hulscher, Saskia, Menge, Wiro M. P. B., Gelens, Edith, Snip, Erwin, Bakker, Remko A., Celanire, Sylvain, Gillard, Michel, Talaga, Patri

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 63 KB

english, 2004

19

Inhibitors of Sir2: Evaluation of Splitomicin Analogues

Posakony, Jeff, Hirao, Maki, Stevens, Sam, Simon, Julian A., Bedalov, Antonio

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 137 KB

english, 2004

20

Synthesis and Evaluation of Oxazaborolidines for Antibacterial Activity against Streptococcus mutans

Jabbour, Adel, Steinberg, Doron, Dembitsky, Valery M., Moussaieff, Arieh, Zaks, Batia, Srebnik, Morris

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 36 KB

english, 2004

21

4-( ω -(Alkyloxy)alkyl)-1 H -imidazole Derivatives as Histamine H 3 Receptor Antagonists/Agonists

Meier, Galina, Krause, Michael, Hüls, Annette, Ligneau, Xavier, Pertz, Heinz H., Arrang, Jean-Michel, Ganellin, C. Robin, Schwartz, Jean-Charles, Schunack, Walter, Stark, Holger

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 131 KB

english, 2004

22

[1-(3,5-Difluoro-4-hydroxyphenyl)-1 H -pyrrol-3-yl]phenylmethanone as a Bioisostere of a Carboxylic Acid Aldose Reductase Inhibitor

Nicolaou, Ioannis, Zika, Chariklia, Demopoulos, Vassilis J.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 52 KB

english, 2004

23

Synthesis and Use of Novel Ether Phospholipid Enantiomers To Probe the Molecular Basis of the Antitumor Effects of Alkyllysophospholipids: Correlation of Differential Activation of c-Jun NH 2 -Terminal Protein Kinase with Antiproliferative Effects in Neuronal Tumor Cells

Samadder, Pranati, Bittman, Robert, Byun, Hoe-Sup, Arthur, Gilbert

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 81 KB

english, 2004

24

Reducing the Peptidyl Features of Caspase-3 Inhibitors: A Structural Analysis

Becker, Joseph W., Rotonda, Jennifer, Soisson, Stephen M., Aspiotis, Renee, Bayly, Christopher, Francoeur, Sébastien, Gallant, Michel, Garcia-Calvo, Marga, Giroux, Andre, Grimm, Erich, Han, Yongxin, M

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 546 KB

english, 2004

25

Drug Discovery Strategies and Methods Edited by Alexandros Makriyannis and Diane Biegel. Marcel Dekker, New York. 2004. xi + 348 pp. 16 × 23.5 cm. ISBN 0-8247-0691-9. $174.00.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 15 KB

english, 2004

26

N -Phenylphenylglycines as Novel Corticotropin Releasing Factor Receptor Antagonists

Molteni, Valentina, Penzotti, Julie, Wilson, Dean M., Termin, Andreas P., Mao, Long, Crane, Christine M., Hassman, Fred, Wang, Tao, Wong, Harvey, Miller, Keith J., Grossman, Scott, Grootenhuis, Peter

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 79 KB

english, 2004

27

Prediction of Biological Targets Using Probabilistic Neural Networks and Atom-Type Descriptors

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 52 KB

english, 2004

28

Significant Differences in Biological Parameters between Prodrugs Cleavable by Carboxypeptidase G2 That Generate 3,5-Difluoro-phenol and -aniline Nitrogen Mustards in Gene-Directed Enzyme Prodrug Therapy Systems

Niculescu-Duvaz, I., Scanlon, I., Niculescu-Duvaz, D., Friedlos, F., Martin, J., Marais, R., Springer, C. J.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 127 KB

english, 2004

29

Design and Synthesis of α-Aryloxy-α-methylhydrocinnamic Acids: A Novel Class of Dual Peroxisome Proliferator-Activated Receptor α/γ Agonists

Xu, Yanping, Rito, Christopher J., Etgen, Garret J., Ardecky, Robert J., Bean, James S., Bensch, William R., Bosley, Jacob R., Broderick, Carol L., Brooks, Dawn A., Dominianni, Samuel J., Hahn, Patric

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 94 KB

english, 2004

30

Synthesis of 2,4-Diamino-6-[2‘- O -(ω-carboxyalkyl)oxydibenz[ b , f ]azepin-5-yl]methylpteridines as Potent and Selective Inhibitors of Pneumocystis c arinii, Toxoplasma g ondii , and Mycobacterium a vium Dihydrofolate Reductase

Rosowsky, Andre, Fu, Hongning, Chan, David C. M., Queener, Sherry F.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 286 KB

english, 2004

31

Novel N- Arylpyrazolo[3,2- c ]-Based Ligands for the Glucocorticoid Receptor: Receptor Binding and in Vivo Activity

Ali, Amjad, Thompson, Christopher F., Balkovec, James M., Graham, Donald W., Hammond, Milton L., Quraishi, Nazia, Tata, James R., Einstein, Monica, Ge, Lan, Harris, Georgianna, Kelly, Terri M., Mazur,

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 274 KB

english, 2004

32

Fluoroartemisinin: Trifluoromethyl Analogues of Artemether and Artesunate

Magueur, Guillaume, Crousse, Benoit, Charneau, Sébastien, Grellier, Philippe, Bégué, Jean-Pierre, Bonnet-Delpon, Danièle

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 102 KB

english, 2004

33

Structure−Function Relationships of Multidrug Resistance P-Glycoprotein

Pajeva, Ilza K., Globisch, Christoph, Wiese, Michael

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 487 KB

english, 2004

34

Non-Peptidic Small-Molecule Inhibitors of the Single-Chain Hepatitis C Virus NS3 Protease/NS4A Cofactor Complex Discovered by Structure-Based NMR Screening

Wyss, Daniel F., Arasappan, Ashok, Senior, Mary M., Wang, Yu-Sen, Beyer, Brian M., Njoroge, F. George, McCoy, Mark A.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 712 KB

english, 2004

35

Identification of Opioid Ligands Possessing Mixed μ Agonist/δ Antagonist Activity among Pyridomorphinans Derived from Naloxone, Oxymorphone, and Hydromorphone.

Ananthan, Subramaniam, Khare, Naveen K., Saini, Surendra K., Seitz, Lainne E., Bartlett, Jeffrey L., Davis, Peg, Dersch, Christina M., Porreca, Frank, Rothman, Richard B., Bilsky, Edward J.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 9 KB

english, 2004

36

5-Substituted Derivatives of 6-Halogeno-3-((2-( S )-azetidinyl)methoxy)pyridine and 6-Halogeno-3-((2-( S )-pyrrolidinyl)methoxy)pyridine with Low Picomolar Affinity for α4β2 Nicotinic Acetylcholine Receptor and Wide Range of Lipophilicity: Potential Probes for Imaging with Positron Emission Tomography

Zhang, Yi, Pavlova, Olga A., Chefer, Svetlana I., Hall, Andrew W., Kurian, Varughese, Brown, LaVerne L., Kimes, Alane S., Mukhin, Alexey G., Horti, Andrew G.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 237 KB

english, 2004

37

Hydrolysis in Drug and Prodrug Metabolism. Chemistry, Biochemistry, and Enzymology By Bernard Testa and Joachim M. Mayer. Wiley-VCH, Zürich, Switzerland. 2003. xx + 780 pp. 18 × 24.5 cm. ISBN 3-906390-25-X. $215.00

Duffel, Michael W.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 15 KB

english, 2004

38

Synthesis and Pharmacological Evaluation of 3-(3,4-Dichlorophenyl)-1-indanamine Derivatives as Nonselective Ligands for Biogenic Amine Transporters

Yu, Han, Kim, In Jong, Folk, John E., Tian, Xinrong, Rothman, Richard B., Baumann, Michael H., Dersch, Christina M., Flippen-Anderson, Judith L., Parrish, Damon, Jacobson, Arthur E., Rice, Kenner C.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 234 KB

english, 2004

39

Parallel Solution-Phase Synthesis of Conformationally Restricted Congeners of Pentamidine and Evaluation of Their Antiplasmodial Activities

Mayence, Annie, Vanden Eynde, Jean Jacques, Krogstad, Fran M., Krogstad, Donald J., Cushion, Melanie T., Huang, Tien L.

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 103 KB

english, 2004

40

A New Class of Nonpeptide Bradykinin B 2 Receptor Ligand, Incorporating a 4-Aminoquinoline Framework. Identification of a Key Pharmacophore To Determine Species Difference and Agonist/Antagonist Profile

Sawada, Yuki, Kayakiri, Hiroshi, Abe, Yoshito, Mizutani, Tsuyoshi, Inamura, Noriaki, Asano, Masayuki, Aramori, Ichiro, Hatori, Chie, Oku, Teruo, Tanaka, Hirokazu

Журнал:

Journal of Medicinal Chemistry

Рік:

2004

Мова:

english

Файл:

PDF, 216 KB

english, 2004