Journal of Medicinal Chemistry
Volume 41, Issue 19 (September 10, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

3551-3556

(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: Identification of a Highly Active Inhibitor of Blood Coagulation Factor Xa Kenneth J. Shaw, William J. Guilford, Jerry L. Dallas, Sunil K. Koovakkaat, Margaret A. McCarrick, Amy Liang, David R. Light, and Michael M. Morrissey [Full Article - PDF]

3557-3562

Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3,5-difluoro- 6-[3-(4,5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylglycine (ZK-807834): A Potent, Selective, and Orally Active Inhibitor of the Blood Coagulation Enzyme Factor Xa Gary B. Phillips, Brad O. Buckman, David D. Davey, Keith A. Eagen, William J. Guilford, Josephine Hinchman, Elena Ho, Sunil Koovakkat, Amy Liang, David R. Light, Raju Mohan, Howard P. Ng, Joseph M. Post, Kenneth J. Shaw, Dave Smith, Babu Subramanyam, Mark E. Sullivan, Lan Trinh, Ron Vergona, Janette Walters, Kathy White, Marc Whitlow, Shung Wu, Wei Xu, and Michael M. Morrissey [Full Article - PDF]

3563-3567

Conformationally Constrained 1,3-Diamino Ketones: A Series of Potent Inhibitors of the Cysteine Protease Cathepsin K Robert W. Marquis, Dennis S. Yamashita, Yu Ru, Stephen M. LoCastro, Hye-Ja Oh, Karl F. Erhard, Renee L. DesJarlais, Martha S. Head, Ward W. Smith, Baoguang Zhao, Cheryl A. Janson, Sherin S. Abdel-Meguid, Thaddeus A. Tomaszek, Mark A. Levy, and Daniel F. Veber [Full Article - PDF]

3568-3571

Discovery of Potent, Achiral Matrix Metalloproteinase Inhibitors Stanislaw Pikul, Kelly L. McDow Dunham, Neil G. Almstead, Biswanath De, Michael G. Natchus, Melanie V. Anastasio, Sara J. McPhail, Catherine E. Snider, Yetunde O. Taiwo, Timothy Rydel, C. Michelle Dunaway, Fei Gu, and Glen E. Mieling [Full Article - PDF]

ARTICLES

3572-3581

Prodrugs of Anthracyclines for Use in Antibody-Directed Enzyme Prodrug Therapy Jean-Claude Florent, Xia Dong, Gilbert Gaudel, Sofia Mitaku, Claude Monneret, Jean-Pierre Gesson, Jean-Claude Jacquesy, Martine Mondon, Brigitte Renoux, Solo Andrianomenjanahary, Sylvie Michel, Michel Koch, François Tillequin, Manfred Gerken, Joerg Czech, Rainer Straub, and Klaus Bosslet [Full Article - PDF]

3582-3595

ATP-Citrate Lyase as a Target for Hypolipidemic Intervention. 2. Synthesis and Evaluation of (3R*,5S*)--Substituted-3-carboxy-3,5-dihydroxyalkanoic Acids and Their -Lactone Prodrugs as Inhibitors of the Enzyme in Vitro and in Vivo Andrew D. Gribble, Robert J. Ife, Antony Shaw, David McNair, Christine E. Novelli, Susan Bakewell, Virendra P. Shah, Roland E. Dolle, Pieter H. Groot, Nigel Pearce, John Yates, David Tew, Helen Boyd, Stephen Ashman, Drake S. Eggleston, R. Curtis Haltiwanger, and George Okafo [Full Article - PDF]

3596-3608

Classical/Nonclassical Hybrid Cannabinoids: Southern Aliphatic Chain-Functionalized C-6 Methyl, Ethyl, and Propyl Analogues David J. Drake, Rader S. Jensen, Jakob Busch-Petersen, Joel K. Kawakami, M. Concepcion Fernandez-Garcia, Pusheng Fan, Alexandros Makriyannis, and Marcus A. Tius [Full Article - PDF]

3609-3623

Derivation of a Three-Dimensional Pharmacophore Model of Substance P Antagonists Bound to the Neurokinin-1 Receptor Yasuo Takeuchi, E. F. Berkley Shands, Denise D. Beusen, and Garland R. Marshall [Full Article - PDF]

3624-3634

2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 Melatonin Receptor Partial Agonists, Antagonists, and Putative Inverse Agonists Gilberto Spadoni, Cesarino Balsamini, Annalida Bedini, Giuseppe Diamantini, Barbara Di Giacomo, Andrea Tontini, and Giorgio Tarzia , Marco Mor, Pier Vincenzo Plazzi, and Silvia Rivara , Romolo Nonno, Marilou Pannacci, Valeria Lucini, Franco Fraschini, and Bojidar Michaylov Stankov [Full Article - PDF]

3635-3644

2-Deoxy Derivative Is a Partial Agonist of the Intracellular Messenger Inositol 3,4,5,6-Tetrakisphosphate in the Epithelial Cell Line T84 Marco T. Rudolf, Wen-hong Li, Nora Wolfson, Alexis E. Traynor-Kaplan, and Carsten Schultz [Full Article - PDF]

3645-3654

Synthesis and Antitumor Activity of 4-Aminomethylthioxanthenone and 5-Aminomethylbenzothiopyranoindazole Derivatives Robert B. Perni, Mark P. Wentland, Jianhua I. Huang, Ronald G. Powles, Suzanne Aldous, Kristina M. Klingbeil, A. Danielle Peverly, Ronald G. Robinson, Thomas H. Corbett, Julie L. Jones, Kenneth C. Mattes, James B. Rake, and Susan A. Coughlin [Full Article - PDF]

3655-3663

Biologically Active Oligodeoxyribonucleotides. 5. 5'-End-Substituted d(TGGGAG) Possesses Anti-Human Immunodeficiency Virus Type 1 Activity by Forming a G-Quadruplex Structure Hitoshi Hotoda, Makoto Koizumi, Rika Koga, Masakatsu Kaneko, Kenji Momota, Toshinori Ohmine, Hidehiko Furukawa, Toshinori Agatsuma, Takashi Nishigaki, Junko Sone, Shinya Tsutsumi, Toshiyuki Kosaka, Koji Abe, Satoshi Kimura, and Kaoru Shimada [Full Article - PDF]

3664-3674

Rational Design, Synthesis, and X-ray Structure of Selective Noncovalent Thrombin Inhibitors Jürgen Wagner, Jörg Kallen, Claus Ehrhardt, Jean-Pierre Evenou, and Dieter Wagner [Full Article - PDF]

3675-3683

2-Iminopyrrolidines as Potent and Selective Inhibitors of Human Inducible Nitric Oxide Synthase Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Kam F. Fok, Albert E. Schmelzer, Barnett S. Pitzele, Lydia Swenton, Gina M. Jerome, Christine M. Kornmeier, William M. Moore, Linda F. Branson, Jane R. Connor, Pamela T. Manning, Mark G. Currie, and E. Ann Hallinan [Full Article - PDF]

3684-3689

Reactions of Melatonin and Related Indoles with Free Radicals: A Computational Study Adrián G. Turjanski, Ruth E. Rosenstein, and Darío A. Estrin [Full Article - PDF]

3690-3698

2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: Synthesis, Affinity for Nicotinic Acetylcholine Receptors, and Molecular Modeling Andrei O. Koren, Andrew G. Horti, Alexey G. Mukhin, Daniela Gündisch, Alane S. Kimes, Robert F. Dannals, and Edythe D. London [Full Article - PDF]

3699-3704

A New Series of Highly Potent Growth Hormone-Releasing Peptides Derived from Ipamorelin Michael Ankersen, Nils L. Johansen, Kjeld Madsen, Birgit S. Hansen, Kirsten Raun, Karin Kramer Nielsen, Henning Thgersen, Thomas K. Hansen, Bernd Peschke, Jesper Lau, Behrend F. Lundt, and Peter H. Andersen [Full Article - PDF]

3705-3714

Novel Orally Active Growth Hormone Secretagogues Thomas K. Hansen, Michael Ankersen, Birgit S. Hansen, Kirsten Raun, Karin K. Nielsen, Jesper Lau, Bernd Peschke, Behrend F. Lundt, Henning Thgersen, Nils L. Johansen, Kjeld Madsen, and Peter H. Andersen [Full Article - PDF]

3715-3726

Synthesis and Biological Evaluation of 2-Acyl Analogues of Paclitaxel (Taxol) David G. I. Kingston, Ashok G. Chaudhary, Mahendra D. Chordia, Milind Gharpure, A. A. Leslie Gunatilaka, Paul I. Higgs, John M. Rimoldi, Lakshman Samala, and Prakash G. Jagtap , Paraskevi Giannakakou , Yuan Q. Jiang, Chii M. Lin, and Ernest Hamel , Byron H. Long, Craig R. Fairchild, and Kathy A. Johnston [Full Article - PDF]

3727-3735

Piperazinyl Oxazolidinone Antibacterial Agents Containing a Pyridine, Diazene, or Triazene Heteroaromatic Ring John A. Tucker, Debra A. Allwine, Kevin C. Grega, Michael R. Barbachyn, Jennifer L. Klock, Jenifer L. Adamski, Steven J. Brickner, Douglas K. Hutchinson, Charles W. Ford, Gary E. Zurenko, Robert A. Conradi, Phillip S. Burton, and Randy M. Jensen [Full Article - PDF]

3736-3747

Bicyclic Acylguanidine Na+/H+ Antiporter Inhibitors Manfred Baumgarth, Norbert Beier, and Rolf Gericke [Full Article - PDF]

NOTES

3748-3752

Anthracene-9,10-diones as Potential Anticancer Agents: Bacterial Mutation Studies of Amido-Substituted Derivatives Reveal an Unexpected Lack of Mutagenicity Stanley Venitt, Christopher Crofton-Sleigh, Mavis Agbandje, Terence C. Jenkins, and Stephen Neidle [Full Article - PDF]

3753-3757

Synthesis and Characterization of Heteroarotinoids Demonstrate Structure Specificity Relationships Doris M. Benbrook, Shankar Subramanian, Jonathan B. Gale, Shengquan Liu, Chad W. Brown, Marcus F. Boehm, and K. Darrell Berlin [Full Article - PDF]

BOOK REVIEWS

3758-3758

A Complete Introduction to Modern NMR Spectroscopy By Roger S. Macomber. Wiley Interscience, New York, NY. 1998. xvii + 382 pp. 21.5 × 28 cm. ISBN 0-471-15736-8. $49.95. Horacio F. Olivo [Full Article - PDF]

3758-3758

Receptor-Based Drug Design Edited by Paul Leff. Marcel Dekker, Inc., New York. 1998. xi + 382 pp. 16 × 23 cm. ISBN 0-8247-0162-3. $175.00. Roger M. Pinder [Full Article - PDF]