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COMMUNICATIONS
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1041-1044
Pyrrolidine Inhibitors of Human Cytosolic Phospholipase A2
Kaoru Seno,
Takayuki Okuno,
Koichi Nishi,
Yasushi Murakami,
Fumihiko Watanabe,
Takaharu Matsuura,
Masaaki Wada,
Yasuhiko Fujii,
Masaaki Yamada,
Tomoyuki Ogawa,
Tetsuo Okada,
Hiroshi Hashizume,
Makoto Kii,
Shin-ichiro Hara,
Sanji Hagishita,
Shozo Nakamoto,
Katsutoshi Yamada,
Yukiko Chikazawa,
Masahiko Ueno,
Isao Teshirogi,
Takashi Ono, and
Mitsuaki Ohtani
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1045-1049
Design, Synthesis, and Antimicrobial Activity of 6-O-Substituted Ketolides Active against Resistant Respiratory Tract Pathogens
Yat Sun Or,
Richard F. Clark,
Sanyi Wang,
Daniel T. W. Chu,
Angela M. Nilius,
Robert K. Flamm,
Michael Mitten,
Patty Ewing,
Jeff Alder, and
Zhenkun Ma
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ARTICLES
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1050-1061
Mapping the Melatonin Receptor. 6. Melatonin Agonists and Antagonists Derived from 6H-Isoindolo[2,1-a]indoles, 5,6-Dihydroindolo[2,1-a]isoquinolines, and 6,7-Dihydro-5H-benzo[c]azepino[2,1-a]indoles
Rüdiger Faust,
Peter J. Garratt,
Rob Jones, and
Li-Kuan Yeh
, Andrew Tsotinis and
Maria Panoussopoulou
, Theodora Calogeropoulou
, Muy-Teck Teh and
David Sugden
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1062-1070
Molecular Modeling of the Aldose Reductase-Inhibitor Complex Based on the X-ray Crystal Structure and Studies with Single-Site-Directed Mutants
Suresh B. Singh,
Michael S. Malamas,
Thomas C. Hohman,
Ramaswamy Nilakantan,
Deborah A. Carper, and
Douglas Kitchen
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1071-1084
Histaprodifens: Synthesis, Pharmacological in Vitro Evaluation, and Molecular Modeling of a New Class of Highly Active and Selective Histamine H1-Receptor Agonists
Sigurd Elz,
Kai Kramer,
Heinz H. Pertz,
Heiner Detert,
Anton M. ter Laak,
Ronald Kühne, and
Walter Schunack
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1085-1093
Highly Selective Chiral N-Substituted 3 -[Bis(4'-fluorophenyl)methoxy]tropane Analogues for the Dopamine Transporter: Synthesis and Comparative Molecular Field Analysis
Michael J. Robarge,
Gregory E. Agoston,
Sari Izenwasser,
Theresa Kopajtic,
Clifford George,
Jonathan L. Katz, and
Amy Hauck Newman
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1094-1108
2',6'-Dimethylphenoxyacetyl: A New Achiral High Affinity P3-P2 Ligand for Peptidomimetic-Based HIV Protease Inhibitors
Pierre L. Beaulieu,
Paul C. Anderson,
Dale R. Cameron,
Gilbert Croteau,
Vida Gorys,
Chantal Grand-Maître,
Daniel Lamarre,
Francine Liard,
William Paris,
Louis Plamondon,
François Soucy,
Diane Thibeault,
Dominik Wernic, and
Christiane Yoakim
, Susan Pav and
Liang Tong
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1109-1122
3D-QSAR CoMFA Study on Imidazolinergic I2 Ligands: A Significant Model through a Combined Exploration of Structural Diversity and Methodology
Nicolas Baurin,
Eric Vangrevelinghe,
Luc Morin-Allory,
Jean-Yves Mérour,
Pierre Renard,
Marc Payard,
Gérald Guillaumet, and
Christophe Marot
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1123-1134
Biarylcarbamoylindolines Are Novel and Selective 5-HT2C Receptor Inverse Agonists: Identification of 5-Methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a Potential Antidepressant/Anxiolytic Agent
Steven M. Bromidge,
Steven Dabbs,
David T. Davies,
Susannah Davies,
D. Malcolm Duckworth,
Ian T. Forbes,
Laramie M. Gaster,
Peter Ham,
Graham E. Jones,
Frank D. King,
Keith R. Mulholland,
Damian V. Saunders,
Paul A. Wyman,
Frank E. Blaney,
Stephen E. Clarke,
Thomas P. Blackburn,
Vicky Holland,
Guy A. Kennett,
Sean Lightowler,
Derek N. Middlemiss,
Brenda Trail,
Graham J. Riley, and
Martyn D. Wood
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1135-1142
Investigating Protein-Ligand Interactions with a Mutant FKBP Possessing a Designed Specificity Pocket
Wu Yang,
Leonard W. Rozamus,
Surinder Narula,
Carl T. Rollins,
Ruth Yuan,
Lawrence J. Andrade,
Mary K. Ram,
Thomas B. Phillips,
Marie Rose van Schravendijk,
David Dalgarno,
Tim Clackson, and
Dennis A. Holt
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1143-1148
Artificial Neural Network Applied to Prediction of Fluorquinolone Antibacterial Activity by Topological Methods
José Jaén-Oltra,
Ma Teresa Salabert-Salvador,
Francisco J. García-March,
Facundo Pérez-Giménez, and
Francisco Tomás-Vert
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1149-1157
5-HT Reuptake Inhibitors with 5-HT1B/1D Antagonistic Activity: A New Approach toward Efficient Antidepressants
Lisa Matzen,
Christoph van Amsterdam,
Wilfried Rautenberg,
Hartmut E. Greiner,
Jürgen Harting,
Christoph A. Seyfried, and
Henning Böttcher
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1158-1164
1,2,4-Triazolo[4,3-a]quinoxalin-1-one: A Versatile Tool for the Synthesis of Potent and Selective Adenosine Receptor Antagonists
Vittoria Colotta,
Daniela Catarzi,
Flavia Varano,
Lucia Cecchi,
Guido Filacchioni,
Claudia Martini,
Letizia Trincavelli, and
Antonio Lucacchini
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1165-1172
Anilide Derivatives of an 8-Phenylxanthine Carboxylic Congener Are Highly Potent and Selective Antagonists at Human A2B Adenosine Receptors
Yong-Chul Kim,
Xiao-duo Ji,
Neli Melman,
Joel Linden, and
Kenneth A. Jacobson
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1173-1179
SH2-Directed Ligands of the Lck Tyrosine Kinase
Tae Ryong Lee and
David S. Lawrence
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1180-1186
Doubly Homologated Dihalovinyl and Acetylene Analogues of Adenosine: Synthesis, Interaction with S-Adenosyl-L-homocysteine Hydrolase, and Antiviral and Cytostatic Effects
Stanislaw F. Wnuk,
Carlos A. Valdez,
Jahanzeb Khan,
Priscilla Moutinho,
Morris J. Robins,
Xiaoda Yang,
Ronald T. Borchardt,
Jan Balzarini, and
Erik De Clercq
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1187-1202
Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 1. N-Cyanoguanidine Bioisosteres Possessing in Vivo Bladder Selectivity
John A. Butera,
Madelene M. Antane,
Schuyler A. Antane,
Thomas M. Argentieri,
Chris Freeden,
Russell F. Graceffa,
Bradford H. Hirth,
Douglas Jenkins,
Joseph R. Lennox,
Edward Matelan,
N. Wesley Norton,
Dominick Quagliato,
Jeffrey H. Sheldon,
Walter Spinelli,
Dawn Warga,
Alexandra Wojdan, and
Morgan Woods
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1203-1214
Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 2. Selective and Potent Benzylamino Cyclobutenediones
Adam M. Gilbert,
Madelene M. Antane,
Thomas M. Argentieri,
John A. Butera,
Gerardo D. Francisco,
Chris Freeden,
Eric G. Gundersen,
Russell F. Graceffa,
David Herbst,
Bradford H. Hirth,
Joseph R. Lennox,
Geraldine McFarlane,
N. Wesley Norton,
Dominick Quagliato,
Jeffrey H. Sheldon,
Dawn Warga,
Alexandra Wojdan, and
Morgan Woods
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1215-1222
Further SAR Studies of Piperidine-Based Analogues of Cocaine. 2. Potent Dopamine and Serotonin Reuptake Inhibitors
Amir P. Tamiz,
Jianrong Zhang,
Judith L. Flippen-Anderson,
Mei Zhang,
Kenneth M. Johnson,
Olivier Deschaux,
Srihari Tella, and
Alan P. Kozikowski
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1223-1233
Novel and Selective Calcitonin-Inducing Agents
Adam M. Gilbert,
Stephen Caltabiano,
Denise Roberts,
Sam F. W. Sum,
Gerardo D. Francisco,
Kitae Lim,
Magda Asselin,
John W. Ellingboe,
Yogendra Kharode,
Anna Cannistraci,
Rita Francis,
Mark TrailSmith, and
David Gralnick
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1234-1241
Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs
Jeffrey J. Hale,
Sander G. Mills,
Malcolm MacCoss,
Conrad P. Dorn,
Paul E. Finke,
Richard J. Budhu,
Robert A. Reamer,
Su-Er W. Huskey,
Debra Luffer-Atlas,
Brian J. Dean,
Erin M. McGowan,
William P. Feeney,
Shuet-Hing Lee Chiu,
Margaret A. Cascieri,
Gary G. Chicchi,
Marc M. Kurtz,
Sharon Sadowski,
Elzbieta Ber,
F. David Tattersall,
Nadia M. J. Rupniak,
Angela R. Williams,
Wayne Rycroft,
Richard Hargreaves,
Joseph M. Metzger, and
D. Euan MacIntyre
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BRIEF ARTICLES
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1242-1245
Active Conformations of Neotame and Other High-Potency Sweeteners
D. Eric Walters,
Indra Prakash, and
Nitin Desai
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1246-1249
Methyl-Substituted Dispiro-1,2,4,5-tetraoxanes: Correlations of Structural Studies with Antimalarial Activity
Kevin J. McCullough,
James K. Wood,
Apurba K. Bhattacharjee,
Yuxiang Dong,
Dennis E. Kyle,
Wilbur K. Milhous, and
Jonathan L. Vennerstrom
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ADDITIONS AND CORRECTIONS
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1250-1250
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Enrique Raviña,
Jesús Negreira,
José Cid,
Christian F. Masaguer,
Elizabeth Rosa,
M. Emilia Rivas,
José A. Fontenla,
M. Isabel Loza,
Helena Tristán,
M. Isabel Cadavid,
Ferran Sanz,
Estrella Lozoya,
Angelo Carotti, and
Antonio Carrieri: Conformationally Constrained Butyrophenones with Mixed Dopaminergic (D2) and Serotoninergic (5-HT2A, 5-HT2C) Affinities: Synthesis, Pharmacology, 3D-QSAR, and Molecular Modeling of (Aminoalkyl)benzo- an
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