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COMMUNICATIONS TO THE EDITOR
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2175-2179
| Spiro[1H-indene-1,4'-piperidine] Derivatives As Potent and Selective Non-Peptide Human Somatostatin Receptor Subtype 2 (sst2) Agonists
Lihu Yang,
Liangqin Guo,
Alexander Pasternak,
Ralph Mosley,
Susan Rohrer,
Elizabeth Birzin,
Forrest Foor,
Kang Cheng,
James Schaeffer, and
Arthur A. Patchett
[Full Article -
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2180-2183
| Isochroman-6-carboxamides as Highly Selective 5-HT1D Agonists: Potential New Treatment for Migraine without Cardiovascular Side Effects
Michael D. Ennis,
Nabil B. Ghazal,
Robert L. Hoffman,
Martin W. Smith,
Siusaidh K. Schlachter,
Charles F. Lawson,
Wha Bin Im,
Jeffrey F. Pregenzer,
Kjell A. Svensson,
Richard A. Lewis,
Edward D. Hall,
Dorothy M. Sutter,
Lorri T. Harris, and
Robert B. McCall
[Full Article -
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EXPEDITED ARTICLES
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2184-2193
| Inhibition of in Vitro and in Vivo HIV Replication by a Distamycin Analogue That Interferes with Chemokine Receptor Function: A Candidate for Chemotherapeutic and Microbicidal Application
O. M. Z. Howard,
J. J. Oppenheim,
Melinda G. Hollingshead,
Joseph M. Covey,
J. Bigelow,
J. J. McCormack,
Robert W. Buckheit, Jr.,
David J. Clanton,
Jim A. Turpin, and
William G. Rice
[Full Article -
PDF] |
2194-2200
| Rational Design and Combinatorial Evaluation of Enzyme Inhibitor Scaffolds: Identification of Novel Inhibitors of Matrix Metalloproteinases
Anna Katrin Szardenings,
David Harris,
Stuart Lam,
Lihong Shi,
David Tien,
Yongwen Wang,
Dinesh V. Patel,
Marc Navre, and
David A. Campbell
[Full Article -
PDF] |
2201-2206
| A Pyridoxine Cyclic Phosphate and Its 6-Azoaryl Derivative Selectively Potentiate and Antagonize Activation of P2X1 Receptors
Kenneth A. Jacobson,
Yong-Chul Kim,
Scott S. Wildman,
Arvind Mohanram,
T. Kendall Harden,
José L. Boyer,
Brian F. King, and
Geoffrey Burnstock
[Full Article -
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ARTICLES
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2207-2215
| Synthesis and Characterization of Long Chain Alkyl Acyl Carnitine Esters. Potentially Biodegradable Cationic Lipids for Use in Gene Delivery
Jinkang Wang,
Xin Guo,
Yuhong Xu,
Lee Barron, and
Francis C. Szoka, Jr.
[Full Article -
PDF] |
2216-2226
| Molecular Modeling Studies of the DNA-Topoisomerase I Ternary Cleavable Complex with Camptothecin
Y. Fan,
J. N. Weinstein,
K. W. Kohn,
L. M. Shi, and
Y. Pommier
[Full Article -
PDF] |
2227-2233
| L-Carnitine Esters as "Soft", Broad-Spectrum Antimicrobial Amphiphiles
Menotti Calvani,
Luciana Critelli,
Grazia Gallo,
Fabrizio Giorgi,
Giancarlo Gramiccioli,
Mosè Santaniello,
Nazareno Scafetta,
Maria O. Tinti, and
Francesco De Angelis
[Full Article -
PDF] |
2234-2242
| N2- and C8-Substituted Oligodeoxynucleotides with Enhanced Thrombin Inhibitory Activity in Vitro and in Vivo
Gong-Xin He,
Steven H. Krawczyk,
S. Swaminathan,
Regan G. Shea,
Joseph P. Dougherty,
Terry Terhorst,
Veronica S. Law,
Linda C. Griffin,
Steven Coutré, and
Norbert Bischofberger
[Full Article -
PDF] |
2243-2251
| Benzylimidazolines as h5-HT1B/1D Serotonin Receptor Ligands: A Structure-Affinity Investigation
Ho Law,
Malgorzata Dukat,
Milt Teitler,
David K. H. Lee,
Lucia Mazzocco,
Raj Kamboj,
Vik Rampersad,
Thomas Prisinzano, and
Richard A. Glennon
[Full Article -
PDF] |
2252-2260
| Discovery of a Novel Series of Potent and Selective Substrate-Based Inhibitors of p60c-src Protein Tyrosine Kinase: Conformational and Topographical Constraints in Peptide Design
Josue Alfaro-Lopez,
Wei Yuan,
Brigitte C. Phan,
Jayesh Kamath,
Qiang Lou,
Kit S. Lam, and
Victor J. Hruby
[Full Article -
PDF] |
2261-2267
| Three-Dimensional Quantitative Structure-Activity Relationship Study of Nonsteroidal Estrogen Receptor Ligands Using the Comparative Molecular Field Analysis/Cross-Validated r2-Guided Region Selection Approach
Beth R. Sadler,
Sung Jin Cho,
Khalid S. Ishaq,
Kun Chae, and
Kenneth S. Korach
[Full Article -
PDF] |
2268-2277
| 7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as Novel Inhibitors of Human Eosinophil Phosphodiesterase
Allen J. Duplantier,
Catharine J. Andresen,
John B. Cheng,
Victoria L. Cohan,
Christian Decker,
Frank M. DiCapua,
Kenneth G. Kraus,
Kerry L. Johnson,
Claudia R. Turner,
John P. UmLand,
John W. Watson,
Ronald T. Wester,
Alison S. Williams, and
John A. Williams
[Full Article -
PDF] |
2278-2288
| Synthesis and Glutathione S-Transferase Structure-Affinity Relationships of Nonpeptide and Peptidase-Stable Glutathione Analogues
Philippe Klotz,
Amal Slaoui-Hasnaoui,
Jean-Louis Banères,
Jean-Frédéric Duckert, and
Jean-Claude Rossi
, Abdelali Kerbal
[Full Article -
PDF] |
2289-2301
| Synthesis and Evaluation of Diphenyl Phosphonate Esters as Inhibitors of the Trypsin-like Granzymes A and K and Mast Cell Tryptase
Delwin S. Jackson,
Stephanie A. Fraser,
Li-Ming Ni,
Chih-Min Kam,
Ulrike Winkler,
David A. Johnson,
Christopher J. Froelich,
Dorothy Hudig, and
James C. Powers
[Full Article - PDF] |
2302-2307
| Studies on Selectin Blockers. 6. Discovery of Homologous Fucose Sugar Unit Necessary for E-Selectin Binding
Yasuyuki Hiramatsu,
Hideki Moriyama,
Takao Kiyoi,
Takahiro Tsukida,
Yoshimasa Inoue, and
Hirosato Kondo
[Full Article - PDF] |
2308-2318
| Synthesis and Antitumor Activity of Ring A- and F-Modified Hexacyclic Camptothecin Analogues
Masamichi Sugimori,
Akio Ejima,
Satoru Ohsuki,
Kouichi Uoto,
Ikuo Mitsui,
Yasuyoshi Kawato,
Yasuhide Hirota,
Keiki Sato, and
Hirofumi Terasawa
[Full Article -
PDF] |
2319-2332
| Comprehensive Study on Structure-Activity Relationships of Rifamycins: Discussion of Molecular and Crystal Structure and Spectroscopic and Thermochemical Properties of Rifamycin O
Alessia Bacchi and
Giancarlo Pelizzi
, Marino Nebuloni and
Pietro Ferrari
[Full Article -
PDF] |
2333-2338
| Structure-Activity Requirements for Flavone Cytotoxicity and Binding to Tubulin
John A. Beutler,
Ernest Hamel,
Arnold J. Vlietinck,
Achiel Haemers,
Padinchare Rajan,
James N. Roitman,
John H. Cardellina II, and
Michael R. Boyd
[Full Article - PDF] |
2339-2344
| Auxiliary Agents for the Peroral Administration of Peptide and Protein Drugs: Synthesis and Evaluation of Novel Pepstatin Analogues
Martin Kratzel,
Romana Hiessböck, and
Andreas Bernkop-Schnürch
[Full Article - PDF] |
2345-2360
| GPIIb/IIIa Integrin Antagonists with the New Conformational Restriction Unit, Trisubstituted  -Amino Acid Derivatives, and a Substituted Benzamidine Structure
Yoshio Hayashi,
Jun Katada,
Takeo Harada,
Akira Tachiki,
Kiyoko Iijima,
Yoshimi Takiguchi,
Michiko Muramatsu,
Hiroshi Miyazaki,
Tohru Asari,
Takeo Okazaki,
Yoshimi Sato,
Emiko Yasuda,
Mako Yano,
Isao Uno, and
Iwao Ojima
[Full Article - PDF] |
2361-2370
| Synthesis and Quantitative Structure-Activity Relationships of N-(1-Benzylpiperidin-4-yl)phenylacetamides and Related Analogues as Potent and Selective  1 Receptor Ligands
Yunsheng Huang,
Philip S. Hammond,
Brian R Whirrett,
Ross J. Kuhner,
Li Wu,
Steven R. Childers, and
Robert H. Mach
[Full Article - PDF] |
2371-2379
| Syntheses and Anticholinesterase Activities of (3aS)-N,N8-Bisnorphenserine, (3aS)-N1,N8-Bisnorphysostigmine, Their Antipodal Isomers, and Other Potential Metabolites of Phenserine
Qian-sheng Yu,
Nigel H. Greig, and
Harold W. Holloway
, Arnold Brossi
[Full Article - PDF] |
2380-2389
| 2-Substituted Analogues of 4'-Iodococaine: Synthesis and Dopamine Transporter Binding Potencies
Kwasi S. Avor,
Satendra Singh,
Thomas W. Seale,
Buddy Pouw, and
Garo P. Basmadjian
[Full Article - PDF] |
2390-2410
| Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. 2. Identification and Structure-Activity Relationships of a Novel Series of N-Alkyl-N-(heteroaryl-substituted benzyl)-N'-arylureas
Akira Tanaka,
Takeshi Terasawa,
Hiroyuki Hagihara,
Yuri Sakuma,
Noriko Ishibe,
Masae Sawada,
Hisashi Takasugi, and
Hirokazu Tanaka
[Full Article - PDF] |
2411-2423
| Nonsymmetric P2/P2' Cyclic Urea HIV Protease Inhibitors. Structure-Activity Relationship, Bioavailability, and Resistance Profile of Monoindazole-Substituted P2 Analogues
George V. De Lucca,
Ui T. Kim,
Jing Liang,
Beverly Cordova,
Ronald M. Klabe,
Sena Garber,
Lee T. Bacheler,
Gilbert N. Lam,
Matthew R. Wright,
Kelly A. Logue,
Susan Erickson-Viitanen,
Soo S. Ko, and
George L. Trainor
[Full Article - PDF] |
NOTES
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2424-2429
| Optimizing the Binding of Fullerene Inhibitors of the HIV-1 Protease through Predicted Increases in Hydrophobic Desolvation
Simon H. Friedman,
Padma S. Ganapathi,
Yves Rubin, and
George L. Kenyon
[Full Article - PDF] |
2430-2435
| Synthesis and Dopamine Transporter Affinity of the Four Stereoisomers of (±)-2-(Methoxycarbonyl)-7-methyl-3-phenyl-7-azabicyclo[2.2.1]heptane
Chunming Zhang,
Sari Izenwasser,
Jonathan L. Katz,
Phyllis D. Terry, and
Mark L. Trudell
[Full Article - PDF] |
2436-2438
| Antimycobacterial Activity of Substituted Isosteres of Pyridine- and Pyrazinecarboxylic Acids
Gerald A. Wächter,
Matt C. Davis,
Arnold R. Martin, and
Scott G. Franzblau
[Full Article - PDF] |