Table of Contents
January 17, 2002
Volume 45, Issue 2
Pages 251-540
Letters
Looking for Selectivity among Cytochrome P450s Inhibitors
Andrea Cavalli and Maurizio Recanatini
pp 251–254Publication Date (Web): December 20, 2001 (Letter)
DOI: 10.1021/jm015567k
Hi-Res PDFBacteriopurpurinimides: Highly Stable and Potent Photosensitizers for Photodynamic Therapy
Yihui Chen, Andrew Graham, William Potter, Janet Morgan, Lurine Vaughan, David A. Bellnier, Barbara W. Henderson, Allan Oseroff, Thomas J. Dougherty, and Ravindra K. Pandey
pp 255–258Publication Date (Web): December 18, 2001 (Letter)
DOI: 10.1021/jm010400c
Design of Substrate-Based Inhibitors of Human β-Secretase
Jay S. Tung, David L. Davis, John P. Anderson, Don E. Walker, Shumeye Mamo, Nancy Jewett, Roy K. Hom, Sukanto Sinha, Eugene D. Thorsett, and Varghese John
pp 259–262Publication Date (Web): December 20, 2001 (Letter)
DOI: 10.1021/jm0155695
Articles
Inhibition of nNOS Activity in Rat Brain by Synthetic Kynurenines: Structure−Activity Dependence
Encarnación Camacho, Josefa León, Adoración Carrión, Antonio Entrena, Germaine Escames, Huda Khaldy, Darío Acuña-Castroviejo, Miguel A. Gallo, and Antonio Espinosa
pp 263–274Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm010916w
Antagonistic Effects of Human Cyclic MBP87-99 Altered Peptide Ligands in Experimental Allergic Encephalomyelitis and Human T-Cell Proliferation
Theodore Tselios, Vasso Apostolopoulos, Ioanna Daliani, Spyros Deraos, Simona Grdadolnik, Thomas Mavromoustakos, Maria Melachrinou, Sotiria Thymianou, Lesley Probert, Athanasia Mouzaki, and John Matsoukas
pp 275–283Publication Date (Web): December 15, 2001 (Article)
DOI: 10.1021/jm0102147
Carbonic Anhydrase Activators: High Affinity Isozymes I, II, and IV Activators, Incorporating a β-Alanyl-histidine Scaffold
Andrea Scozzafava and Claudiu T. Supuran
pp 284–291Publication Date (Web): December 20, 2001 (Article)
DOI: 10.1021/jm010958k
Structure−Activity Relationships of the Antimalarial Agent Artemisinin. 6. The Development of Predictive In Vitro Potency Models Using CoMFA and HQSAR Methodologies
Mitchell A. Avery, Maria Alvim-Gaston, Carlos R. Rodrigues, Eliezer J. Barreiro, Fred E. Cohen, Yogesh A. Sabnis, and John R. Woolfrey
pp 292–303Publication Date (Web): December 08, 2001 (Article)
DOI: 10.1021/jm0100234
Graphical Model for Estimating Oral Bioavailability of Drugs in Humans and Other Species from Their Caco-2 Permeability and in Vitro Liver Enzyme Metabolic Stability Rates
Arun K. Mandagere, Thomas N. Thompson, and Kin-Kai Hwang
pp 304–311Publication Date (Web): December 20, 2001 (Article)
DOI: 10.1021/jm010152k
Carbonic Anhydrase Inhibitors: Anticonvulsant Sulfonamides Incorporating Valproyl and Other Lipophilic Moieties
Bernard Masereel, Stéphanie Rolin, Francesco Abbate, Andrea Scozzafava, and Claudiu T. Supuran
pp 312–320Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm0109199
Synthesis, Structure, and Activity of Diclofenac Analogues as Transthyretin Amyloid Fibril Formation Inhibitors
Vibha B. Oza, Craig Smith, Prakash Raman, Edward K. Koepf, Hilal A. Lashuel, H. Mike Petrassi, Kyle P. Chiang, Evan T. Powers, James Sachettinni, and Jeffery W. Kelly
pp 321–332Publication Date (Web): December 20, 2001 (Article)
DOI: 10.1021/jm010257n
Elucidating the Inhibiting Mode of AHPBA Derivatives against HIV-1 Protease and Building Predictive 3D-QSAR Models
Xaioqin Huang, Liaosa Xu, Xiaomin Luo, Kangnian Fan, Ruyun Ji, Gang Pei, Kaixian Chen, and Hualiang Jiang
pp 333–343Publication Date (Web): December 08, 2001 (Article)
DOI: 10.1021/jm0102710
Pyrrolo[1,3]benzothiazepine-Based Atypical Antipsychotic Agents. Synthesis, Structure−Activity Relationship, Molecular Modeling, and Biological Studies
Giuseppe Campiani, Stefania Butini, Sandra Gemma, Vito Nacci, Caterina Fattorusso, Bruno Catalanotti, Gianluca Giorgi, Alfredo Cagnotto, Mara Goegan, Tiziana Mennini, Patrizia Minetti, M. Assunta Di Cesare, Domenico Mastroianni, Nazzareno Scafetta, Bruno Galletti, M. Antonietta Stasi, Massimo Castorina, Licia Pacifici, Orlando Ghirardi, Ornella Tinti, and Paolo Carminati
pp 344–359Publication Date (Web): December 08, 2001 (Article)
DOI: 10.1021/jm010982y
Design, Synthesis, and Preliminary Pharmacological Evaluation of N-Acyl-3-aminoglutarimides as Broad-Spectrum Chemokine Inhibitors in Vitro and Anti-inflammatory Agents in Vivo
David J. Fox, Jill Reckless, Stuart G. Warren, and David J. Grainger
pp 360–370Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm010984i
β-Strand Mimicking Macrocyclic Amino Acids: Templates for Protease Inhibitors with Antiviral Activity
Matthew P. Glenn, Leonard K. Pattenden, Robert C. Reid, David P. Tyssen, Joel D. A. Tyndall, Christopher J. Birch, and David P. Fairlie
pp 371–381Publication Date (Web): December 12, 2001 (Article)
DOI: 10.1021/jm010414i
2-Amino-3-aroyl-4,5-alkylthiophenes: Agonist Allosteric Enhancers at Human A1 Adenosine Receptors
C. Elisabet Tranberg, Andrea Zickgraf, Brian N. Giunta, Henning Luetjens, Heidi Figler, Lauren J. Murphree, Ruediger Falke, Holger Fleischer, Joel Linden, Peter J. Scammells, and Ray. A. Olsson
pp 382–389Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm010081p
C-7 Analogues of Progesterone as Potent Inhibitors of the P-Glycoprotein Efflux Pump
Fabio Leonessa, Ji-Hyun Kim, Alem Ghiorghis, Robert J. Kulawiec, Charles Hammer, Abdelhossein Talebian, and Robert Clarke
pp 390–398Publication Date (Web): December 14, 2001 (Article)
DOI: 10.1021/jm010126m
New Approach to Pharmacophore Mapping and QSAR Analysis Using Inductive Logic Programming. Application to Thermolysin Inhibitors and Glycogen Phosphorylase b Inhibitors
Nathalie Marchand-Geneste, Kimberly A. Watson, Bjørn K. Alsberg, and Ross D. King
pp 399–409Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm0155244
Synthesis, Biological Evaluation, and Quantitative Structure−Activity Relationship Analysis of New Schiff Bases of Hydroxysemicarbazide as Potential Antitumor Agents
Shijun Ren, Rubin Wang, Kenichi Komatsu, Patricia Bonaz-Krause, Yegor Zyrianov, Charles E. McKenna, Csaba Csipke, Zoltan A. Tokes, and Eric J. Lien
pp 410–419Publication Date (Web): December 07, 2001 (Article)
DOI: 10.1021/jm010252q
2,5‘-Disubstituted Adenosine Derivatives: Evaluation of Selectivity and Efficacy for the Adenosine A1, A2A, and A3 Receptor
Erica W. van Tilburg, Jacobien von Frijtag Drabbe Künzel, Miriam de Groote, and Ad P. IJzerman
pp 420–429Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm010952v
A New Type of Mixed Anhydride and Its Applications to the Synthesis of 7-Substituted 8-Chloro-5,5-dioxoimidazo[1,2-b][1,4,2]benzodithiazines with in Vitro Antitumor Activity
Zdzisław Brzozowski and Franciszek Sa̧czewski
pp 430–437Publication Date (Web): December 06, 2001 (Article)
DOI: 10.1021/jm010953n
Novel Spiropiperidines as Highly Potent and Subtype Selective σ-Receptor Ligands. Part 1
Christoph A. Maier and Bernhard Wünsch
pp 438–448Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm010992z
Water-Soluble, Core-Modified Porphyrins as Novel, Longer-Wavelength-Absorbing Sensitizers for Photodynamic Therapy. II. Effects of Core Heteroatoms and Meso-Substituents on Biological Activity
David G. Hilmey, Masako Abe, Marina I. Nelen, Corey E. Stilts, Gary A. Baker, Sheila N. Baker, Frank V. Bright, Sherry R. Davies, Sandra O. Gollnick, Allan R. Oseroff, Scott L. Gibson, Russell Hilf, and Michael R. Detty
pp 449–461Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm0103662
Synthesis and Characterization of a Series of Novel Monoacylated Ascorbic Acid Derivatives, 6-O-Acyl-2-O-α-d-glucopyranosyl-l-ascorbic Acids, as Skin Antioxidants
Itaru Yamamoto, Akihiro Tai, Yoshihito Fujinami, Kenji Sasaki, and Shino Okazaki
pp 462–468Publication Date (Web): December 15, 2001 (Article)
DOI: 10.1021/jm010379f
Radiolabeling and In Vivo Behavior of Copper-64-Labeled Cross-Bridged Cyclam Ligands
Xiankai Sun, Melinda Wuest, Gary R. Weisman, Edward H. Wong, David P. Reed, C. Andrew Boswell, Ramunas Motekaitis, Arthur E. Martell, Michael J. Welch, and Carolyn J. Anderson
pp 469–477Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm0103817
Structure−Activity Profiles of Complex Biantennary Glycans with Core Fucosylation and with/without Additional α2,3/α2,6 Sialylation: Synthesis of Neoglycoproteins and Their Properties in Lectin Assays, Cell Binding, and Organ Uptake
Carlo Unverzagt, Sabine André, Joachim Seifert, Shuji Kojima, Christian Fink, Geetha Srikrishna, Hudson Freeze, Klaus Kayser, and Hans-Joachim Gabius
pp 478–491Publication Date (Web): December 20, 2001 (Article)
DOI: 10.1021/jm0110237
4-(Phenylsulfonyl)piperidines: Novel, Selective, and Bioavailable 5-HT2A Receptor Antagonists
Stephen R. Fletcher, Frank Burkamp, Peter Blurton, Susan K. F. Cheng, Robert Clarkson, Desmond O'Connor, Daniel Spinks, Matthew Tudge, Monique B. van Niel, Smita Patel, Kerry Chapman, Rose Marwood, Sara Shepheard, Graham Bentley, Gina P Cook, Linda J Bristow, Jose L. Castro, Peter H. Hutson, and Angus M. MacLeod
pp 492–503Publication Date (Web): December 20, 2001 (Article)
DOI: 10.1021/jm011030v
Carbonic Anhydrase Activators: Design of High Affinity Isozymes I, II, and IV Activators, Incorporating Tri-/Tetrasubstituted-pyridinium-azole Moieties
Monica Ilies, Mircea D. Banciu, Marc A. Ilies, Andrea Scozzafava, Miron T. Caproiu, and Claudiu T. Supuran
pp 504–510Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm011031n
Orally-Effective, Long-Acting Sorbitol Dehydrogenase Inhibitors: Synthesis, Structure−Activity Relationships, and in Vivo Evaluations of Novel Heterocycle-Substituted Piperazino-Pyrimidines
Margaret Y. Chu-Moyer, William E. Ballinger, David A. Beebe, Richard Berger, James B. Coutcher, Wesley W. Day, Jiancheng Li, Banavara L. Mylari, Peter J. Oates, and R. Matthew Weekly
pp 511–528Publication Date (Web): December 20, 2001 (Article)
DOI: 10.1021/jm010440g
Brief Articles
Aldisine Alkaloids from the Philippine Sponge Stylissa massa Are Potent Inhibitors of Mitogen-Activated Protein Kinase Kinase-1 (MEK-1)
Deniz Tasdemir, Robert Mallon, Michael Greenstein, Larry R. Feldberg, Steven C. Kim, Karen Collins, Donald Wojciechowicz, Gina C. Mangalindan, Gisela P. Concepción, Mary Kay Harper, and Chris M. Ireland
pp 529–532Publication Date (Web): December 15, 2001 (Brief Article)
DOI: 10.1021/jm0102856
Design, Synthesis, and Pharmacological Evaluation of New Farnesyl Protein Transferase Inhibitors
Raymond Houssin, Jean Pommery, Marie-Catherine Salaün, Sophie Deweer, Jean-François Goossens, Philippe Chavatte, and Jean-Pierre Hénichart
pp 533–536Publication Date (Web): December 08, 2001 (Brief Article)
DOI: 10.1021/jm010297r
4‘-Arylpyrrolomorphinans: Effect of a Pyrrolo-N-benzyl Substituent in Enhancing δ-Opioid Antagonist Activity
Sanjay K. Srivastava, Stephen M. Husbands, Mario D. Aceto, Carl N. Miller, John R. Traynor, and John W. Lewis
pp 537–540Publication Date (Web): December 19, 2001 (Brief Article)
DOI: 10.1021/jm010841w