Bioorganic & Medicinal Chemistry Letters Vol. 13, No. 6
Contents vii
Contributors to this Issue
979
Graphical Abstracts
J. M. Evans, B. A. Turner, S. Bowen, A. M. Ho, R. W. Sarver, E. Benson and C. N. Parker
993
Inhibition of Bacterial IF2 Binding to FMet-tRNA(fMet) by Aminoglycosides
C. Lherbet, M. Morin, R. Castonguay and J. W. Keillor
997
Synthesis of Aza and Oxaglutamyl-p-nitroanilide Derivatives and Their Kinetic Studies with g-Glutamyltranspeptidase
C. Che, G. Petit, F. Kotzyba-Hibert, S. Bertrand, D. Bertrand, T. Grutter and M. Goeldner
1001
Syntheses and Biological Properties of Cysteine-Reactive Epibatidine Derivatives
D. Vullo, M. Franchi, E. Gallori, J. Pastorek, A. Scozzafava, S. Pastorekova and C. T. Supuran
1005
Carbonic Anhydrase Inhibitors: Inhibition of the Tumor-Associated Isozyme IX with Aromatic and Heterocyclic Sulfonamides
K. Prokai-Tatrai, V. Nguyen, A. D. Zharikova, A. C. Braddy, S. M. Stevens, Jr. and L. Prokai
1011
Prodrugs to Enhance Central Nervous System Effects of the TRH-like Peptide pGlu-Glu-Pro-NH2
D. J. Burdick, K. Paris, K. Weese, M. Stanley, 1015 M. Beresini, K. Clark, R. S. McDowell, J. C. Marsters, Jr. and T. R. Gadek
N-Benzoyl Amino Acids as LFA-1/ICAM Inhibitors 1: Amino Acid Structure–Activity Relationship
W. Yang, J. Yan, G. Springsteen, S. Deeter and 1019 B. Wang
A Novel Type of Fluorescent Boronic Acid That Shows Large Fluorescence Intensity Changes Upon Binding with a Carbohydrate in Aqueous Solution at Physiological pH
M. L. Quan, C. D. Ellis, M. Y. He, A. Y. Liauw, P. Y. S. Lam, K. A. Rossi, R. M. Knabb, J. M. Luettgen, M. R. Wright, P. C. Wong and R. R. Wexler
1023
Nonbenzamidine Isoxazoline Derivatives as Factor Xa Inhibitors
J. J. Kiddle, H. J. McCreery and S. Soles
1029
Synthesis and Binding Affinity of Neuropeptide Y at Opiate Receptors
Q. Zhu, D. B. Li, M. Uttamchandani and S. Q. Yao
1033
Facile Synthesis of 7-Amino-4-carbamoylmethylcoumarin (ACC)Containing Solid Supports and Their Corresponding Fluorogenic Protease Substrates
A. Tanaka and T. Nishizaki
1037
The Newly Synthesized Linoleic Acid Derivative FR236924 Induces a Long-Lasting Facilitation of Hippocampal Neurotransmission by Targeting Nicotinic Acetylcholine Receptors
M. Abdel-Aziz, T. Yamasaki and M. Otsuka
1041
Synthesis and Hybridization Property of Novel 20 ,50 -isoDNA Mimic Chiral Peptide Nucleic Acids
M. Yoshikawa, F. Xu, T. Morikawa, K. Ninomiya and H. Matsuda
1045
Anastatins A and B, New Skeletal Flavonoids with Hepatoprotective Activities from the Desert Plant Anastatica hierochuntica
R. Jain, B. Vaitilingam, A. Nayyar and P. B. Palde
1051
Substituted 4-Methylquinolines as a New Class of Anti-Tuberculosis Agents
I. T. Forbes, D. G. Cooper, E. K. Dodds, S. E. Douglas, A. D. Gribble, R. J. Ife, A. P. Lightfoot, M. Meeson, L. P. Campbell, T. Coleman, G. J. Riley and D. R. Thomas
1055
Identification of a Novel Series of Selective 5-HT7 Receptor Antagonists
M. Rodriguez, D. Bonnet-Delpon, J.-P. Be´gue´, 1059 A. Robert and B. Meunier
Alkylation of Manganese(II) Tetraphenylporphyrin by Antimalarial Fluorinated Artemisinin Derivatives
1063
a-Selective Glycosylation with 5-Thioglucopyranosyl Donors; Synthesis of an Isomaltotetraoside Mimic Composed of 5-Thioglucopyranose Units
J. A. Blackie, J. C. Bloomer, M. J. B. Brown, 1067 H.-Y. Cheng, B. Hammond, D. M. B. Hickey, R. J. Ife, C. A. Leach, V. A. Lewis, C. H. Macphee, K. J. Milliner, K. E. Moores, I. L. Pinto, S. A. Smith, I. G. Stansfield, S. J. Stanway, M. A. Taylor and C. J. Theobald
The Identification of Clinical Candidate SB-480848: A Potent Inhibitor of Lipoprotein-Associated Phospholipase A2
K. Urbahns, M. Ha¨rter, A. Vaupel, M. Albers, 1071 D. Schmidt, U. Bru¨ggemeier, B. Stelte-Ludwig, C. Gerdes and H. Tsujishita
Biphenyls as Potent Vitronectin Receptor Antagonists. Part 2: Biphenylalanine Ureas
Q. Cheng, H. Kiyota, M. Yamaguchi, T. Horiguchi and T. Oritani
1075
Synthesis and Biological Evaluation of 4-Deacetoxy-1,7-dideoxy Azetidine Paclitaxel Analogues
M. S. Han and D. H. Kim
1079
Visual Detection of AMP and Real-Time Monitoring of Cyclic Nucleotide Phosphodiesterase (PDE) Activity in Neutral Aqueous Solution. Chemosensor-Coupled Assay of PDE and PDE Inhibitors
A. Basak, S. Mandal and S. Bandyopadhyay
1083
Regioselective Hydrolysis of Pentaacetyl Catechin and Epicatechin by Porcine Liver Esterase
J. Lee, S. E. Kim, J. Y. Lee, S. Y. Kim, S. U. Kang, S. H. Seo, M. W. Chun, T. Kang, S. Y. Choi and H. O. Kim
1087
N-Alkoxysulfamide, N-Hydroxysulfamide, and Sulfamate Analogues of Methionyl and Isoleucyl Adenylates as Inhibitors of Methionyl-tRNA and Isoleucyl-tRNA Synthetases
1093 J. E. Tellew, R. A. F. Baska, S. M. Beyer, K. E. Carlson, L. A. Cornelius, L. Fadnis, Z. Gu, B. L. Kunst, M. C. Kowala, H. Monshizadegan, N. Murugesan, C. S. Ryan, M. T. Valentine, Y. Yang and J. E. Macor
Discovery of 40 -[(Imidazol-1-yl)methyl]biphenyl-2-sulfonamides as Dual Endothelin/Angiotensin II Receptor Antagonists
1097
Synthesis and Antibacterial Study of 10, 15, 20-Triphenyl-5-{4-hydroxy-3(trimethylammonium)methyl}phenylporphyrin as Models for Combination of Porphyrin and Alkylating Agent
H. Matsuda, Y. Pongpiriyadacha, T. Morikawa, 1101 A. Kishi, S. Kataoka and M. Yoshikawa
Protective Effects of Steroid Saponins from Paris polyphylla var. yunnanensis on Ethanol- or Indomethacin-Induced Gastric Mucosal Lesions in Rats: Structural Requirement for Activity and Mode of Action
A. Cooke, A. Anderson, J. Bennett, K. Buchanan, D. Gemmell, N. Hamilton, M. Maidment, P. McPhail, D. Stevenson and H. Sundaram
1107
Novel a-Amino-Acid Phenolic Ester Derivatives with Intravenous Anaesthetic Activity
W. Han, Z. Hu, X. Jiang, Z. R. Wasserman and C. P. Decicco
1111
Glycine a-Ketoamides as HCV NS3 Protease Inhibitors
T. Terasaka, I. Nakanishi, K. Nakamura, Y. Eikyu, T. Kinoshita, N. Nishio, A. Sato, M. Kuno, N. Seki and K. Sakane
1115
Structure-Based De Novo Design of Non-nucleoside Adenosine Deaminase Inhibitors
1119 A. A. Rahman, M. K. Daoud, M. Dukat, K. Herrick-Davis, A. Purohit, M. Teitler, A. T. do Amaral, A. Malvezzi and R. A. Glennon
Conformationally-Restricted Analogues and Partition Coefficients of the 5-HT3 Serotonin Receptor Ligands meta-Chlorophenylbiguanide (mCPBG) and meta-Chlorophenylguanidine (mCPG)
1125
Preparation of Potential Inhibitors of the Mur-Pathway Enzymes on Solid Support Using an Acetal Linker
X. Billot, A. Chateauneuf, N. Chauret, D. Denis, 1129 G. Greig, M.-C. Mathieu, K. M. Metters, D. M. Slipetz and R. N. Young
Discovery of a Potent and Selective Agonist of the Prostaglandin EP4 Receptor
H. Matsuda, K. Ohara, Y. Morii, M. Hashimoto, K. Miyairi and T. Okuno
J. Zhang, X. Wu, X. Cao, F. Yang, J. Wang, X. Zhou and X.-L. Zhang
M. Maletic, J. Antonic, A. Leeman, G. Santorelli and S. Waddell
R. N. Misra, D. B. Rawlins, H. Xiao, W. Shan, I. Bursuker, K. A. Kellar, J. G. Mulheron, J. S. Sack, J. S. Tokarski, S. D. Kimball and K. R. Webster
1133
1H-Pyrazolo[3,4-b]pyridine Inhibitors of Cyclin-Dependent Kinases
1137 T. D. Penning, N. S. Chandrakumar, B. N. Desai, S. W. Djuric, A. F. Gasiecki, J. W. Malecha, J. M. Miyashiro, M. A. Russell, L. J. Askonas, J. K. Gierse, E. I. Harding, M. K. Highkin, J. F. Kachur, S. H. Kim, D. Villani-Price, E. Y. Pyla, N. S. Ghoreishi-Haack and W. G. Smith
Synthesis of Imidazopyridines and Purines as Potent Inhibitors of Leukotriene A4 Hydrolase
G. Semple, B.-M. Andersson, V. Chhajlani, J. Georgsson, M. J. Johansson, A˚. Rosenquist and L. Swanson
1141
Synthesis and Biological Activity of Kappa Opioid Receptor Agonists. Part 2: Preparation of 3-Aryl-2-pyridone Analogues Generated by Solution- and Solid-Phase Parallel Synthesis Methods
A. Zamri, I. J. Schalk, F. Pattus and M. A. Abdallah
1147
Bacterial Siderophores: Synthesis and Biological Activities of Novel Pyochelin Analogues
P.-E. Sum, D. How, N. Torres, P. J. Petersen, 1151 E. B. Lenoy, W. J. Weiss and T. S. Mansour X. Zhang, A. C. Schmitt, W. Jiang, Z. Wasserman and C. P. Decicco
1157
Novel Ether Derivatives of Mannopeptimycin Glycopeptide Antibiotic Design and Synthesis of Potent, Non-peptide Inhibitors of HCV NS3 Protease
S. Miao, J. Bao, M. L. Garcia, J. L. Goulet, 1161 X. J. Hong, G. J. Kaczorowski, F. Kayser, G. C. Koo, A. Kotliar, W. A. Schmalhofer, K. Shah, P. J. Sinclair, R. S. Slaughter, M. S. Springer, M. J. Staruch, N. N. Tsou, F. Wong, W. H. Parsons and K. M. Rupprecht
Benzamide Derivatives as Blockers of Kv1.3 Ion Channel
J. W. Butcher, N. J. Liverton, D. A. Claremon, 1165 R. M. Freidinger, N. K. Jurkiewicz, J. J. Lynch, J. J. Salata, J. Wang, C. M. Dieckhaus, D. E. Slaughter and K. Vyas
Novel 5-Cyclopropyl-1,4-benzodiazepin-2-ones as Potent and Selective IKs-Blocking Class III Antiarrhythmic Agents
J. Wanner, D. Tang, C. C. McComas, B. M. Crowley, W. Jiang, J. Moss and D. L. Boger
1169
A New and Improved Method for Deglycosidation of Glycopeptide Antibiotics Exemplified with Vancomycin, Ristocetin, and Ramoplanin
L. Zhao, M. K. O’Reilly, M. D. Shultz and J. Chmielewski
1175
Interfacial Peptide Dimerization
Inhibitors
of
HIV-1
Integrase
Activity
and
V. I. Lodyato, I. L. Yurkova, V. L. Sorokin, 1179 O. I. Shadyro, V. I. Dolgopalets and M. A. Kisel
Synthesis and Properties of 11-(3,5-Di-tert-butyl-2-hydroxyphenylcarbamoyl)undecanoic Acid, a New Amphiphilic Antioxidant
J. D. Speake, F. Navas, III, M. J. Bishop, D. T. Garrison, E. C. Bigham, S. J. Hodson, D. L. Saussy, J. A. Liacos, P. E. Irving and B. W. Sherman
1183
2-(Anilinomethyl)imidazolines as a1 Adrenergic Receptor Agonists: a1a Subtype Selective 20 -Heteroaryl Compounds
J. Shi, Z. Xiao, M. A. Ihnat, C. Kamat, B. Pandit, Z. Hu and P.-K. Li
1187
Structure–Activity Relationships Studies of the Anti-Angiogenic Activities of Linomide
Z. Wan, J. C. Boehm, M. J. Bower, S. Kassis, 1191 J. C. Lee, B. Zhao and J. L. Adams
N-Phenyl-N-purin-6-yl Ureas: The Design and Synthesis of P38a MAP Kinase Inhibitors
1195
3,4-Diaryl-5-hydroxyfuranones: Highly Selective Inhibitors of Cyclooxygenase-2 with Aqueous Solubility
W. C. Black, C. Brideau, C.-C. Chan, S. Charleson, W. Cromlish, R. Gordon, E. L. Grimm, G. Hughes, S. Leger, C.-S. Li, D. Riendeau, M. The´rien, Z. Wang, L.-J. Xu and P. Prasit
1199 R. J. Mattson, J. D. Catt, D. Keavy, C. P. Sloan, J. Epperson, Q. Gao, D. B. Hodges, L. Iben, C. D. Mahle, E. Ryan and F. D. Yocca
Indanyl Piperazines as Melatonergic MT2 Selective Agents
O. B. Wallace, D. W. Smith, M. S. Deshpande, 1203 C. Polson and K. M. Felsenstein
Inhibitors of Ab Production: Solid-Phase Synthesis and SAR of a-Hydroxycarbonyl Derivatives
A. V. Stachulski, F. Scheinmann, J. R. Ferguson, 1207 J. L. Law, K. W. Lumbard, P. Hopkins, N. Patel, S. Clarke, A. Gloyne and S. P. Joel
Structure–Activity Relationships of Some Opiate Glycosides
X. Zhang, G. C. G. Pais, E. S. Svarovskaia, 1215 C. Marchand, A. A. Johnson, R. G. Karki, M. C. Nicklaus, V. K. Pathak, Y. Pommier and T. R. Burke, Jr. I
Azido-Containing Aryl b-Diketo Acid HIV-1 Integrase Inhibitors
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