Table of Contents
May 8, 2003
Volume 46, Issue 10
Pages 1775-2016
Perspectives
2002 Medicinal Chemistry Division Award Address: Monoamine Transporters and Opioid Receptors. Targets for Addiction Therapy
F. Ivy Carroll
pp 1775–1794Publication Date (Web): April 09, 2003 (Perspective)
DOI: 10.1021/jm030092d
Hi-Res PDF Letters
Synthesis and Antibacterial Activity of 6-O-Arylbutynyl Ketolides with Improved Activity against Some Key Erythromycin-Resistant Pathogens
Robert F. Keyes, Justin J. Carter, Erika E. Englund, Melissa M. Daly, Greg G. Stone, Angela M. Nilius, and Zhenkun Ma
pp 1795–1798Publication Date (Web): April 15, 2003 (Letter)
DOI: 10.1021/jm025580k
Design and Synthesis of Statine-Based Cell-Permeable Peptidomimetic Inhibitors of Human β-Secretase
Roy K. Hom, Larry Y. Fang, Shumeye Mamo, Jay S. Tung, Ashley C. Guinn, Don E. Walker, David L. Davis, Andrea F. Gailunas, Eugene D. Thorsett, Sukanto Sinha, Jeroen E. Knops, Nancy E. Jewett, John P. Anderson, and Varghese John
pp 1799–1802Publication Date (Web): April 11, 2003 (Letter)
DOI: 10.1021/jm025619l
Benzodiazepines as Potent and Selective Bradykinin B1 Antagonists
Michael R. Wood, June J. Kim, Wei Han, Bruce D. Dorsey, Carl F. Homnick, Robert M. DiPardo, Scott D. Kuduk, Tanya MacNeil, Kathy L. Murphy, Edward V. Lis, Richard W. Ransom, Gary L. Stump, Joseph J. Lynch, Stacey S. O'Malley, Patricia J. Miller, Tsing-Bau Chen, Charles M. Harrell, Raymond S. L. Chang, Punam Sandhu, Joan D. Ellis, Peter J. Bondiskey, Douglas J. Pettibone, Roger M. Freidinger, and Mark G. Bock
pp 1803–1806Publication Date (Web): April 03, 2003 (Letter)
DOI: 10.1021/jm034020y
Retroinverso Analogue of the Antiviral Octapeptide C8 Inhibits Feline Immunodeficiency Virus in Serum
Anna Maria D'Ursi, Simone Giannecchini, Armida Di Fenza, Cinzia Esposito, Maria Rosaria Armenante, Alfonso Carotenuto, Mauro Bendinelli, and Paolo Rovero
pp 1807–1810Publication Date (Web): April 12, 2003 (Letter)
DOI: 10.1021/jm034012h
Articles
Design, Synthesis, and Evaluation of Benzothiadiazepine Hydroxamates as Selective Tumor Necrosis Factor-α Converting Enzyme Inhibitors
Robert J. Cherney, James J.-W. Duan, Matthew E. Voss, Lihua Chen, Li Wang, Dayton T. Meyer, Zelda R. Wasserman, Karl D. Hardman, Rui-Qin Liu, Maryanne B. Covington, Mingxin Qian, Sandhya Mandlekar, David D. Christ, James M. Trzaskos, Robert C. Newton, Ronald L. Magolda, Ruth R. Wexler, and Carl P. Decicco
pp 1811–1823Publication Date (Web): April 02, 2003 (Article)
DOI: 10.1021/jm020475w
Novel Pyrazolo[3,4-d]pyrimidine-Based Inhibitors of Staphlococcus aureus DNA Polymerase III: Design, Synthesis, and Biological Evaluation
Amjad Ali, Gayle E. Taylor, Ken Ellsworth, Georgianna Harris, Ronald Painter, Lynn L. Silver, and Katherine Young
pp 1824–1830Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm020483c
Design, Synthesis, and Biological Evaluation of Monopyrrolinone-Based HIV-1 Protease Inhibitors
Amos B. Smith, III, Louis-David Cantin, Alexander Pasternak, Lisa Guise-Zawacki, Wenquin Yao, Adam K. Charnley, Joseph Barbosa, Paul A. Sprengeler, Ralph Hirschmann, Sanjeev Munshi, David B. Olsen, William A. Schleif, and Lawrence C. Kuo
pp 1831–1844Publication Date (Web): April 09, 2003 (Article)
DOI: 10.1021/jm0204587
Rational Design, Synthesis, and Structure−Activity Relationships of Novel Factor Xa Inhibitors: (2-Substituted-4-amidinophenyl)pyruvic and -propionic Acids1
Kazuyuki Sagi, Tadakiyo Nakagawa, Masahiro Yamanashi, Shingo Makino, Mitsuo Takahashi, Masaru Takayanagi, Kaoru Takenaka, Nobuyasu Suzuki, Seiji Oono, Noriyasu Kataoka, Kohki Ishikawa, Sayaka Shima, Yumiko Fukuda, Takashi Kayahara, Shunji Takehana, Yoichiro Shima, Kazumi Tashiro, Hiroshi Yamamoto, Ryota Yoshimoto, Seinosuke Iwata, Takashi Tsuji, Kuniya Sakurai, and Masataka Shoji
pp 1845–1857Publication Date (Web): April 11, 2003 (Article)
DOI: 10.1021/jm020485x
Effects of Heterocyclic Aromatic Substituents on Binding Affinities at Two Distinct Sites of Somatostatin Receptors. Correlation with the Electrostatic Potential of the Substituents
Vidya Prasad, Elizabeth T. Birzin, Cheryl T. McVaugh, Rachel D. van Rijn, Susan P. Rohrer, Gary Chicchi, Dennis J. Underwood, Edward R. Thornton, Amos B. Smith, III, and Ralph Hirschmann
pp 1858–1869Publication Date (Web): April 15, 2003 (Article)
DOI: 10.1021/jm0205088
2-Amino-3-benzoylthiophene Allosteric Enhancers of A1 Adenosine Agonist Binding: New 3, 4-, and 5-Modifications
Henning Lütjens, Andrea Zickgraf, Heidi Figler, Joel Linden, Ray A. Olsson, and Peter J. Scammells
pp 1870–1877Publication Date (Web): April 12, 2003 (Article)
DOI: 10.1021/jm020295m
Antiviral Amphipathic Oligo- and Polyribonucleotides: Analogue Development and Biological Studies
Robyn M. Hyde, Arthur D. Broom, and Robert W. Buckheit, Jr.
pp 1878–1885Publication Date (Web): April 04, 2003 (Article)
DOI: 10.1021/jm0203276
Synthesis and Evaluation of B-, C-, and D-Ring-Substituted Estradiol Carboxylic Acid Esters as Locally Active Estrogens
David C. Labaree, Jing-xin Zhang, Heather A. Harris, Craig O'Connor, Toni Y. Reynolds, and Richard B. Hochberg
pp 1886–1904Publication Date (Web): April 05, 2003 (Article)
DOI: 10.1021/jm0204340
A Novel Antibacterial 8-Chloroquinolone with a Distorted Orientation of the N1-(5-Amino-2,4-difluorophenyl) Group
Yasuhiro Kuramoto, Yoshihiro Ohshita, Jiro Yoshida, Akira Yazaki, Motoo Shiro, and Tohru Koike
pp 1905–1917Publication Date (Web): April 09, 2003 (Article)
DOI: 10.1021/jm0205090
Design of Selective Peptidomimetic Agonists for the Human Orphan Receptor BRS-3
Dirk Weber, Claudia Berger, Peter Eickelmann, Jochen Antel, and Horst Kessler
pp 1918–1930Publication Date (Web): April 15, 2003 (Article)
DOI: 10.1021/jm0210921
Inhibition of Papilloma Formation by Analogues of 7,8-Dihydroretinoic Acid
Y. Fulmer Shealy, James M. Riordan, Jerry L. Frye, Linda Simpson-Herren, Brahma P. Sani, and Donald L. Hill
pp 1931–1939Publication Date (Web): April 12, 2003 (Article)
DOI: 10.1021/jm020324t
Molecular Modeling Calculations of HIV-1 Reverse Transcriptase Nonnucleoside Inhibitors: Correlation of Binding Energy with Biological Activity for Novel 2-Aryl-Substituted Benzimidazole Analogues
Marilyn B. Kroeger Smith, Brian M. Hose, Arie Hawkins, James Lipchock, David W. Farnsworth, Robert C. Rizzo, Julian Tirado-Rives, Edward Arnold, Wanyi Zhang, Stephen H. Hughes, William L. Jorgensen, Christopher J. Michejda, and Richard H. Smith, Jr.
pp 1940–1947Publication Date (Web): April 11, 2003 (Article)
DOI: 10.1021/jm020271f
Structural Properties of Dibenzosuberanylpiperazine Derivatives for Efficient Reversal of Chloroquine Resistance in Plasmodium chabaudi
Yumiko Osa, Seiki Kobayashi, Yoko Sato, Yumiko Suzuki, Kouichi Takino, Tsutomu Takeuchi, Yoshiyuki Miyata, Masakazu Sakaguchi, and Hiroaki Takayanagi
pp 1948–1956Publication Date (Web): April 02, 2003 (Article)
DOI: 10.1021/jm020379v
Antimalarial Activity of Novel 1,2,5,6-Tetraoxacycloalkanes and 1,2,5-Trioxacycloalkanes
Hye-Sook Kim, Khurshida Begum, Naoki Ogura, Yusuke Wataya, Yuji Nonami, Toyonari Ito, Araki Masuyama, Masatomo Nojima, and Kevin J. McCullough
pp 1957–1961Publication Date (Web): April 03, 2003 (Article)
DOI: 10.1021/jm020387b
Synthesis and Biological Evaluation of New 2-(4,5-Dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine Derivatives
Frédérique Touzeau, Axelle Arrault, Gérald Guillaumet, Elizabeth Scalbert, Bruno Pfeiffer, Marie-Claire Rettori, Pierre Renard, and Jean-Yves Mérour
pp 1962–1979Publication Date (Web): April 05, 2003 (Article)
DOI: 10.1021/jm021050c
Cyclopropane-Based Conformational Restriction of Histamine. (1S,2S)-2-(2-Aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a Highly Selective Agonist for the Histamine H3 Receptor, Having a cis-Cyclopropane Structure
Yuji Kazuta, Kazufumi Hirano, Kentaro Natsume, Shizuo Yamada, Ryohei Kimura, Shun-ichiro Matsumoto, Kiyoshi Furuichi, Akira Matsuda, and Satoshi Shuto
pp 1980–1988Publication Date (Web): March 20, 2003 (Article)
DOI: 10.1021/jm020415q
Synthesis and Biological Evaluation of Thiol-Based Inhibitors of Glutamate Carboxypeptidase II: Discovery of an Orally Active GCP II Inhibitor
Pavel Majer, Paul F. Jackson, Greg Delahanty, Brian S. Grella, Yao-Sen Ko, Weixing Li, Qun Liu, Keith M. Maclin, Jana Poláková, Kathryn A Shaffer, Doris Stoermer, Dilrukshi Vitharana, Eric Yanjun Wang, Anthony Zakrzewski, Camilo Rojas, Barbara S. Slusher, Krystyna M. Wozniak, Eric Burak, Tharin Limsakun, and Takashi Tsukamoto
pp 1989–1996Publication Date (Web): April 02, 2003 (Article)
DOI: 10.1021/jm020515w
Biaryl Analogues of Conformationally Constrained Tricyclic Tropanes as Potent and Selective Norepinephrine Reuptake Inhibitors: Synthesis and Evaluation of Their Uptake Inhibition at Monoamine Transporter Sites
Jia Zhou, Ao Zhang, Thomas Kläss, Kenneth M. Johnson, Cheng Z. Wang, Yan Ping Ye, and Alan P. Kozikowski
pp 1997–2007Publication Date (Web): April 08, 2003 (Article)
DOI: 10.1021/jm020596w
Synthesis and Structure−Activity Relationships of cis-Tetrahydrophthalazinone/Pyridazinone Hybrids: A Novel Series of Potent Dual PDE3/PDE4 Inhibitory Agents
Margaretha Van der Mey, Kirsten M. Bommelé, Hildegard Boss, Armin Hatzelmann, Mike Van Slingerland, Geert J. Sterk, and Hendrik Timmerman
pp 2008–2016Publication Date (Web): April 12, 2003 (Article)
DOI: 10.1021/jm030776l