Table of Contents
June 19, 2003
Volume 46, Issue 13
Pages 2551-2794
Award Address
2003 Claude S. Hudson Award Address in Carbohydrate Chemistry. Heparin: Structure and Activity
Robert J. Linhardt
pp 2551–2564Publication Date (Web): May 20, 2003 (Perspective)
DOI: 10.1021/jm030176m
Hi-Res PDF Letters
Deoxyribonucleoside 2‘- or 3‘-Mixed Disulfides: Prodrugs To Target Ribonucleotide Reductase and/or To Inhibit HIV Reverse Transcription
Béatrice Roy, Stéphane Chambert, Michel Lepoivre, Anne-Marie Aubertin, Jan Balzarini, and Jean-Luc Décout
pp 2565–2568Publication Date (Web): May 23, 2003 (Letter)
DOI: 10.1021/jm0256225
Spirocyclopropyl β-Lactams as Mechanism-Based Inhibitors of Serine β-Lactamases. Synthesis by Rhodium-Catalyzed Cyclopropanation of 6-Diazopenicillanate Sulfone
Vincent P. Sandanayaka, Amar S. Prashad, Youjun Yang, R. Thomas Williamson, Yang I. Lin, and Tarek S. Mansour
pp 2569–2571Publication Date (Web): May 23, 2003 (Letter)
DOI: 10.1021/jm034056q
Articles
QSAR and Proteo-chemometric Analysis of the Interaction of a Series of Organic Compounds with Melanocortin Receptor Subtypes
Maris Lapinsh, Peteris Prusis, Ilze Mutule, Felikss Mutulis, and Jarl E. S. Wikberg
pp 2572–2579Publication Date (Web): May 23, 2003 (Article)
DOI: 10.1021/jm020945m
Inhibition of Cdc25 Phosphatases by Indolyldihydroxyquinones
Jungsan Sohn, Brendan Kiburz, Zhitao Li, Liu Deng, Alexias Safi, Michael C. Pirrung, and Johannes Rudolph
pp 2580–2588Publication Date (Web): May 21, 2003 (Article)
DOI: 10.1021/jm0300835
Dual Probes for the Dopamine Transporter and σ1 Receptors: Novel Piperazinyl Alkyl-bis(4‘-fluorophenyl)amine Analogues as Potential Cocaine-Abuse Therapeutic Agents
Jianjing Cao, Santosh S. Kulkarni, Stephen M. Husbands, Wayne D. Bowen, Wanda Williams, Theresa Kopajtic, Jonathan L. Katz, Clifford George, and Amy Hauck Newman
pp 2589–2598Publication Date (Web): May 15, 2003 (Article)
DOI: 10.1021/jm030008u
Characterization of a Series of 3-Amino-2-phenylpropene Derivatives as Novel Bovine Chromaffin Vesicular Monoamine Transporter Inhibitors
Rohan P. Perera, D. Shyamali Wimalasena, and Kandatege Wimalasena
pp 2599–2605Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm030004p
Synthesis and Characterization of the First Fluorescent Antagonists for Human 5-HT4 Receptors
Isabelle Berque-Bestel, Jean-Louis Soulier, Mireille Giner, Lucie Rivail, Michel Langlois, and Sames Sicsic
pp 2606–2620Publication Date (Web): May 14, 2003 (Article)
DOI: 10.1021/jm0307887
Utilization of a β-Aminophosphotyrosyl Mimetic in the Design and Synthesis of Macrocyclic Grb2 SH2 Domain-Binding Peptides
Kyeong Lee, Manchao Zhang, Hongpeng Liu, Dajun Yang, and Terrence R. Burke, Jr.
pp 2621–2630Publication Date (Web): May 22, 2003 (Article)
DOI: 10.1021/jm030049q
Discovery and Structural Modification of Inhibitors of Methionine Aminopeptidases from Escherichia coli and Saccharomyces cerevisiae
Qun-Li Luo, Jing-Ya Li, Zhi-Ying Liu, Ling-Ling Chen, Jia Li, Zhen Qian, Qiang Shen, Yu Li, Gerald H. Lushington, Qi-Zhuang Ye, and Fa-Jun Nan
pp 2631–2640Publication Date (Web): May 22, 2003 (Article)
DOI: 10.1021/jm0300532
The Most Potent Organophosphorus Inhibitors of Leucine Aminopeptidase. Structure-Based Design, Chemistry, and Activity
Jolanta Grembecka, Artur Mucha, Tomasz Cierpicki, and Paweł Kafarski
pp 2641–2655Publication Date (Web): May 20, 2003 (Article)
DOI: 10.1021/jm030795v
Discovery of a Potent and Selective Protein Kinase CK2 Inhibitor by High-Throughput Docking
Eric Vangrevelinghe, Kaspar Zimmermann, Joseph Schoepfer, Robert Portmann, Doriano Fabbro, and Pascal Furet
pp 2656–2662Publication Date (Web): May 21, 2003 (Article)
DOI: 10.1021/jm030827e
Synthesis and Biological Evaluation of N1-(Anthracen-9-ylmethyl)triamines as Molecular Recognition Elements for the Polyamine Transporter
Chaojie Wang, Jean-Guy Delcros, John Biggerstaff, and Otto Phanstiel, IV
pp 2663–2671Publication Date (Web): May 20, 2003 (Article)
DOI: 10.1021/jm030028w
Molecular Requirements for Targeting the Polyamine Transport System. Synthesis and Biological Evaluation of Polyamine−Anthracene Conjugates
Chaojie Wang, Jean-Guy Delcros, John Biggerstaff, and Otto Phanstiel, IV
pp 2672–2682Publication Date (Web): May 20, 2003 (Article)
DOI: 10.1021/jm020598g
Novel (2E,4E,6Z)-7-(2-Alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic Acid Retinoid X Receptor Modulators Are Active in Models of Type 2 Diabetes
P. Y. Michellys, R. J. Ardecky, J. H. Chen, D. L. Crombie, G. J. Etgen, M. M. Faul, A. L. Faulkner, T. A. Grese, R. A. Heyman, D. S. Karanewsky, K. Klausing, M. D. Leibowitz, S. Liu, D. A. Mais, C. M. Mapes, K. B. Marschke, A. Reifel-Miller, K. M. Ogilvie, D. Rungta, A. W. Thompson, J. S. Tyhonas, and M. F. Boehm
pp 2683–2696Publication Date (Web): May 20, 2003 (Article)
DOI: 10.1021/jm020340q
Synthesis and Complement Inhibitory Activity of B/C/D-Ring Analogues of the Fungal Metabolite 6,7-Diformyl-3‘,4‘,4a‘,5‘,6‘,7‘,8‘,8a‘-octahydro-4,6‘,7‘-trihydroxy- 2‘,5‘,5‘,8a‘-tetramethylspiro[1‘(2‘H)-naphthalene-2(3H)-benzofuran]
Barton J. Bradbury, Piotr Bartyzel, Teodoro S. Kaufman, Marcelo J. Nieto, Robert D. Sindelar, Susanne M. Scesney, Bruce R. Gaumond, and Henry C. Marsh, Jr.
pp 2697–2705Publication Date (Web): May 24, 2003 (Article)
DOI: 10.1021/jm0204284
Synthesis and Antibacterial Activity of a Novel Series of Acylides: 3-O-(3-Pyridyl)acetylerythromycin A Derivatives
Tetsuya Tanikawa, Toshifumi Asaka, Masato Kashimura, Keiko Suzuki, Hiroyuki Sugiyama, Masakazu Sato, Kazuya Kameo, Shigeo Morimoto, and Atsushi Nishida
pp 2706–2715Publication Date (Web): May 20, 2003 (Article)
DOI: 10.1021/jm020568d
Synthesis and Biological Evaluation of 18-Methoxycoronaridine Congeners. Potential Antiaddiction Agents
Martin E. Kuehne, Liwen He, Patrick A. Jokiel, C. J. Pace, M. W. Fleck, I. M. Maisonneuve, Stanley D. Glick, and Jean M. Bidlack
pp 2716–2730Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm020562o
Synthesis of Substituted 6-Anilinouracils and Their Inhibition of DNA Polymerase IIIC and Gram-Positive Bacterial Growth
Chengxin Zhi, Zheng-Yu Long, Joseph Gambino, Wei-Chu Xu, Neal C. Brown, Marjorie Barnes, Michelle Butler, William LaMarr, and George E. Wright
pp 2731–2739Publication Date (Web): May 15, 2003 (Article)
DOI: 10.1021/jm020591z
Synthesis and Evaluation of 11C-Labeled 6-Substituted 2-Arylbenzothiazoles as Amyloid Imaging Agents
Chester A. Mathis, Yanming Wang, Daniel P. Holt, Guo-Feng Huang, Manik L. Debnath, and William E. Klunk
pp 2740–2754Publication Date (Web): May 24, 2003 (Article)
DOI: 10.1021/jm030026b
Antiretroviral Activity of Semisynthetic Derivatives of Glycopeptide Antibiotics
Jan Balzarini, Christophe Pannecouque, Erik De Clercq, Andrey Y. Pavlov, Svetlana S. Printsevskaya, Olga V. Miroshnikova, Marina I. Reznikova, and Maria N. Preobrazhenskaya
pp 2755–2764Publication Date (Web): May 24, 2003 (Article)
DOI: 10.1021/jm0300882
SYNOPSIS: SYNthesize and OPtimize System in Silico
H. Maarten Vinkers, Marc R. de Jonge, Frederik F. D. Daeyaert, Jan Heeres, Lucien M. H. Koymans, Joop H. van Lenthe, Paul J. Lewi, Henk Timmerman, Koen Van Aken, and Paul A. J. Janssen
pp 2765–2773Publication Date (Web): May 24, 2003 (Article)
DOI: 10.1021/jm030809x
1-[[(3-Hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: A Potent, Selective, and Orally Bioavailable Dipeptidyl Peptidase IV Inhibitor with Antihyperglycemic Properties
Edwin B. Villhauer, John A. Brinkman, Goli B. Naderi, Bryan F. Burkey, Beth E. Dunning, Kapa Prasad, Bonnie L. Mangold, Mary E. Russell, and Thomas E. Hughes
pp 2774–2789Publication Date (Web): May 24, 2003 (Article)
DOI: 10.1021/jm030091l
Brief Articles
Conformationally Constrained Analogues of Diacylglycerol. 19. Synthesis and Protein Kinase C Binding Affinity of Diacylglycerol Lactones Bearing an N-Hydroxylamide Side Chain
Yongseok Choi, Ji-Hye Kang, Nancy E. Lewin, Peter M. Blumberg, Jeewoo Lee, and Victor E. Marquez
pp 2790–2793Publication Date (Web): May 22, 2003 (Brief Article)
DOI: 10.1021/jm030082c
Additions and Corrections
Conformationally Constrained Analogues of Diacylglycerol. 18. The Incorporation of a Hydroxamate Moiety into Diacylglycerol-Lactones Reduces Lipophilicity and Helps Discriminate between sn-1 and sn-2 Binding Modes to Protein Kinase C (PK-C). Implications for Isozyme Specificity.
Jeewoo Lee, Kee-Chung Han, Ji-Hye Kang, Larry L. Pearce, Nancy E. Lewin, Shunqi Yan, Samira Benzaria, Marc C. Nicklaus, Peter M. Blumberg, and Victor E. Marquez:
p 2794Publication Date (Web): May 22, 2003 (Addition/Correction)
DOI: 10.1021/jm030167d