Journal of Medicinal Chemistry
Volume 41, Issue 7 (March 26, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

1007-1010

Physicochemical High Throughput Screening: Parallel Artificial Membrane Permeation Assay in the Description of Passive Absorption Processes Manfred Kansy, Frank Senner, and Klaus Gubernator [Full Article - PDF]

EXPEDITED ARTICLES

1011-1013

Design of Novel, Potent, Noncovalent Inhibitors of Thrombin with Nonbasic P-1 Substructures: Rapid Structure-Activity Studies by Solid-Phase Synthesis William C. Lumma, Jr., Keith M. Witherup, Thomas J. Tucker, Steven F. Brady, John T. Sisko, Adel M. Naylor-Olsen, S. Dale Lewis, Bobby J. Lucas, and Joseph P. Vacca [Full Article - PDF]

ARTICLES

1014-1026

Cytotoxic Activities of Mannich Bases of Chalcones and Related Compounds Jonathan R. Dimmock, N. Murthi Kandepu, Mark Hetherington, J. Wilson Quail, Uma Pugazhenthi, Athena M. Sudom, Mahmood Chamankhah, Patricia Rose, Eric Pass, Theresa M. Allen, Sarah Halleran, Jen Szydlowski, Bulent Mutus, Marie Tannous, Elias K. Manavathu, Timothy G. Myers, Erik De Clercq,O and Jan BalzariniO [Full Article - PDF]

1027-1033

Thiol-Induced Nitric Oxide Release from 3-Halogeno-3,4-dihydrodiazete 1,2-Dioxides Igor A. Kirilyuk, Darkhan I. Utepbergenov, Dmitrii G. Mazhukin, Klaus Fechner, Katharina Mertsch, Valery V. Khramtsov, Ingolf E. Blasig, and Reiner F. Haseloff [Full Article - PDF]

1034-1041

Design and Synthesis of Enantiomers of 3,5-Dinitro-o-tyrosine: -Amino-3-hydroxy-5-methyl-4-isoxazolepropanoic Acid (AMPA) Receptor Antagonists Guoping Sun, Meri Slavica, Norman J. Uretsky, Lane J. Wallace, Gamal Shams, David M. Weinstein, John C. Miller, and Duane D. Miller [Full Article - PDF]

1042-1049

Novel Nonpeptide CCK-B Antagonists: Design and Development of Quinazolinone Derivatives as Potent, Selective, and Orally Active CCK-B Antagonists Janak K. Padia, Mark Field, Joanna Hinton, Ken Meecham, Julius Pablo, Rob Pinnock, Bruce D. Roth, Lakhbir Singh, Nirmala Suman-Chauhan, Bharat K. Trivedi, and Louise Webdale [Full Article - PDF]

1050-1059

Inhibition of Fc-eps-RI-Mediated Activation of Mast Cells by 2,3,4-Trihydropyrimidino[2,1-a]isoquinolines Dieter Scholz, Hannelore Schmidt, Eva E. Prieschl, Robert Csonga, Winfried Scheirer, Virginia Weber, Anna Lembachner, Gunther Seidl, Gudrun Werner, Peter Mayer, and Thomas Baumruker [Full Article - PDF]

1060-1067

2-Amino-4H-3,1-benzoxazin-4-ones as Inhibitors of C1r Serine Protease Sheryl J. Hays, Bradley W. Caprathe, John L. Gilmore, Nilam Amin, Mark R. Emmerling, Walter Michael, Ravi Nadimpalli, Rathna Nath, Kadee J. Raser, Daniel Stafford, Desiree Watson, Kevin Wang, and Juan C. Jaen [Full Article - PDF]

1068-1083

Steroidal and Nonsteroidal Sulfamates as Potent Inhibitors of Steroid Sulfatase L. W. Lawrence Woo, Nicola M. Howarth, Atul Purohit, Hatem A. M. Hejaz, Michael J. Reed, and Barry V. L. Potter [Full Article - PDF]

1084-1091

Novel 5-(3-Aryl-2-propynyl)-5-(arylsulfonyl)thiazolidine-2,4-diones as Antihyperglycemic Agents Jay Wrobel, Zenan Li, Arlene Dietrich, Michael McCaleb, Brenda Mihan, Janet Sredy, and Donald Sullivan [Full Article - PDF]

1092-1098

Synthesis and Endectocidal Activity of Novel 1-(Arylsulfonyl)-1-[(trifluoromethyl)sulfonyl]methane Derivatives David I. Wickiser, Sharon A. Wilson, Daniel E. Snyder, Karl R. Dahnke, Charles K. Smith II, and Paul J. McDermott [Full Article - PDF]

1099-1111

Novel Synthetic Inhibitors of Selectin-Mediated Cell Adhesion: Synthesis of 1,6-Bis[3-(3-carboxymethylphenyl)-4-(2--D-mannopyranosyloxy)phenyl]hexane (TBC1269) Timothy P. Kogan, Brian Dupré, Huong Bui, Kathy L. McAbee, Jamal M. Kassir, Ian L. Scott, Xin Hu, Peter Vanderslice, Pamela J. Beck, and Richard A. F. Dixon [Full Article - PDF]

1112-1123

New Cyclooxygenase-2/5-Lipoxygenase Inhibitors. 1. 7-tert-Butyl-2,3-dihydro-3,3-dimethylbenzofuran Derivatives as Gastrointestinal Safe Antiinflammatory and Analgesic Agents: Discovery and Variation of the 5-Keto Substituent John M. Janusz, Patricia A. Young, James M. Ridgeway, Michael W. Scherz, Kevin Enzweiler, Laurence I. Wu, Lixian Gan, Renuka Darolia, Randall S. Matthews, Duane Hennes, David E. Kellstein, Shelley A. Green, Jennifer L. Tulich, Theresa Rosario-Jansen, I. Jack Magrisso, Kenneth R. Wehmeyer, Deborah L. Kuhlenbeck, Thomas H. Eichhold, Roy L. M. Dobson, Steven P. Sirko, and Ralph W. Farmer [Full Article - PDF]

1124-1137

New Cyclooxygenase-2/5-Lipoxygenase Inhibitors. 2. 7-tert-Butyl-2,3-dihydro-3,3-dimethylbenzofuran Derivatives as Gastrointestinal Safe Antiinflammatory and Analgesic Agents: Variations of the Dihydrobenzofuran Ring John M. Janusz, Patricia A. Young, Michael W. Scherz, Kevin Enzweiler, Laurence I. Wu, Lixian Gan, Stanislaw Pikul, Kelly L. McDow-Dunham, Carl R. Johnson, C. B. Senanayake, David E. Kellstein, Shelley A. Green, Julie L. Tulich, Theresa Rosario-Jansen, I. Jack Magrisso, Kenneth R. Wehmeyer, Deborah L. Kuhlenbeck, Thomas H. Eichhold, and Roy L. M. Dobson [Full Article - PDF]

1138-1145

Synthesis and Anticonvulsant Activity of 2(3H)-Benzoxazolone and 2(3H)-Benzothiazolone Derivatives Huseyin Ucar, Kim Van derpoorten, Silvia Cacciaguerra, Santi Spampinato, James P. Stables, Paul Depovere, Majed Isa, Bernard Masereel, Jacques Delarge, and Jacques H. Poupaert [Full Article - PDF]

1146-1154

Potent Antagonists of Somatostatin: Synthesis and Biology Simon J. Hocart, Rahul Jain, William A. Murphy, John E. Taylor, Barry Morgan, and David H. Coy [Full Article - PDF]

1155-1162

Antitumor Agents. 181. Synthesis and Biological Evaluation of 6,7,2',3',4'-Substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a New Class of Antimitotic Antitumor Agents Yi Xia, Zheng-Yu Yang, Peng Xia, Kenneth F. Bastow, Yoko Tachibana, Sheng-Chu Kuo, Ernest Hamel, Torben Hackl, and Kuo-Hsiung Lee [Full Article - PDF]

1163-1171

Synthesis and Evaluation of Compounds That Facilitate the Gastrointestinal Absorption of Heparin Andrea Leone-Bay, Duncan R. Paton, John Freeman, Christine Lercara, Doris O'Toole, David Gschneidner, Eric Wang, Elizabeth Harris, Connie Rosado, Theresa Rivera, Aldonna DeVincent, Monica Tai, Frank Mercogliano, Rajesh Agarwal, Harry Leipold, and Robert A. Baughman [Full Article - PDF]

1172-1184

(3R,4S)-3-[4-(4-Fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: A Conformationally Restricted Analogue of the NR2B Subtype-Selective NMDA Antagonist (1S,2S)-1-(4-Hydroxyphenyl)-2- (4-hydroxy-4-phenylpiperidino)-1-propanol Todd W. Butler, James F. Blake, Jon Bordner, Paul Butler, Bertrand L. Chenard, Mary A. Collins, Debra DeCosta, Mary J. Ducat, Michael E. Eisenhard, Frank S. Menniti, Martin J. Pagnozzi, Steven B. Sands, Barbara E. Segelstein, Walter Volberg, W. Frost White, and Dayao Zhao [Full Article - PDF]

1185-1194

Role of the C(6)-Hydroxy Group in Bicyclomycin: Synthesis, Structure, and Chemical, Biochemical, and Biological Properties Alejandro Santillán, Jr., Xiangdong Zhang, Jon Hardesty, William R. Widger, and Harold Kohn [Full Article - PDF]

NOTES

1195-1200

Pharmacophoric Requirements for Cannabinoid Side Chains: Multiple Bond and C1'-Substituted 8-Tetrahydrocannabinols Demetris P. Papahatjis, Therapia Kourouli, Vasiliki Abadji, Andreas Goutopoulos, and Alexandros Makriyannis [Full Article - PDF]

1201-1204

Simultaneous Measurement of Nineteen Binding Constants of Peptides to Vancomycin Using Affinity Capillary Electrophoresis-Mass Spectrometry Yuriy M. Dunayevskiy, Yelena V. Lyubarskaya, Yen-Ho Chu, Paul Vouros, and Barry L. Karger [Full Article - PDF]