Volume 13; Issue 10

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Bioorganic & Medicinal Chemistry Letters
Volume 13; Issue 10

Bioorganic & Medicinal Chemistry Letters

Volume 13; Issue 10

1

A novel bicyclic ketolide derivative

Ying Zhao, Qidong You, Wenbin Shen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 157 KB

english, 2003

2

Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches

Robert A Pearlstein, Roy J Vaz, Jiesheng Kang, Xiao-Liang Chen, Maria Preobrazhenskaya, Andrey E Shchekotikhin, Alexander M Korolev, Ludmila N Lysenkova, Olga V Miroshnikova, James Hendrix, David Ramp

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 333 KB

english, 2003

3

Anti-AIDS agents 54. A potent anti-HIV chalcone and flavonoids from genus Desmos

Jiu-Hong Wu, Xi-Hong Wang, Yang-Hua Yi, Kuo-Hsiung Lee

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 135 KB

english, 2003

4

Structure–activity relationship of a novel class of naphthyl amide KATP channel openers

Sean C Turner, William A Carroll, Tammie K White, Michael E Brune, Steven A Buckner, Murali Gopalakrishnan, Adebola Fabiyi, Michael J Coghlan, Victoria E Scott, Neil A Castle, Anthony V Daza, Ivan Mil

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 175 KB

english, 2003

5

Photoinduced cleavage of DNA by bromofluoroacetophenone–pyrrolecarboxamide conjugates

Paul A. Wender, Raok Jeon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 205 KB

english, 2003

6

Unique spirocyclopiperazinium salt. Part 2: synthesis and structure–activity relationship of dispirocyclopiperazinium salts as analgesics

Xin Wang, Feng-Li Gao, Hong-Bin Piao, Tie-Ming Cheng, Run-Tao Li

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 158 KB

english, 2003

7

Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives

Franck Augé, William Hornebeck, Martine Decarme, Jean-Yves Laronze

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 191 KB

english, 2003

8

Synthesis and in vivo imaging properties of [11C]befloxatone: A novel highly potent positron emission tomography ligand for mono-amine oxidase-A

Frédéric Dolle, Héric Valette, Yann Bramoulle, Ilonka Guenther, Chantal Fuseau, Christine Coulon, Carole Lartizien, Samir Jegham, Pascal George, Olivier Curet, Jean-Louis Pinquier, Michel Bottlaender

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 219 KB

english, 2003

9

4-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists

Bernd Büttelmann, Alexander Alanine, Anne Bourson, Ramanjit Gill, Marie-Paule Heitz, Vincent Mutel, Emmanuel Pinard, Gerhard Trube, René Wyler

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 169 KB

english, 2003

10

New fibrinolytic agents: benzothiophene derivatives as inhibitors of the t-PA–PAI-1 complex formation

Guillaume De Nanteuil, Christine Lila-Ambroise, Alain Rupin, Marie-Odile Vallez, Tony J Verbeuren

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 168 KB

english, 2003

11

Synthesis and pharmacological activity of fluorescent histamine H2 receptor antagonists related to potentidine

Liantao Li, Julia Kracht, Shiqi Peng, Günther Bernhardt, Sigurd Elz, Armin Buschauer

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 183 KB

english, 2003

12

Solid-Phase synthesis of endothelin receptor antagonists

Udo E.W Lange, Wilfried M Braje, Willi Amberg, Georg Kettschau

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 181 KB

english, 2003

13

Discovery of novel low molecular weight inhibitors of IMPDH via virtual needle screening

Stephen D Pickett, Bradley S Sherborne, Trevor Wilkinson, James Bennett, Neera Borkakoti, Michael Broadhurst, David Hurst, Ian Kilford, Murray McKinnell, Philip S Jones

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 212 KB

english, 2003

14

Design, synthesis and biological evaluation of hetaryl-nucleoside derivatives as inhibitors of chitin synthase

Jean-Bernard Behr, Thierry Gourlain, Abdellatif Helimi, Georges Guillerm

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 209 KB

english, 2003

15

Anilinopyrimidines as novel antituberculosis agents

Jody Morgan, Rachada Haritakul, Paul A. Keller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 122 KB

english, 2003

16

Synthesis of beta-Lactamase activated nitric oxide donors

Xiaoping Tang, Tingwei Cai, Peng George Wang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 149 KB

english, 2003

17

2,4-Disubstituted pyrimidines: A novel class of KDR kinase inhibitors

Peter J. Manley, Adrienne E. Balitza, Mark T. Bilodeau, Kathleen E. Coll, George D. Hartman, Rosemary C. McFall, Keith W. Rickert, Leonard D. Rodman, Kenneth A. Thomas

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 212 KB

english, 2003

18

Identification of 2-Aminobenzimidazole dimers as antibacterial agents

Punit P Seth, Elizabeth A Jefferson, Lisa M Risen, Stephen A Osgood

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 155 KB

english, 2003

19

Identification of a novel antiangiogenic agent; 4-(N-Imidazol-2-ylmethyl)amino benzopyran analogues

Nakjeong Kim, Sunkyung Lee, Kyu Yang Yi, Sung-eun Yoo, Guncheol Kim, Chong Ock Lee, Sung Hee Park, Byung Ho Lee

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 139 KB

english, 2003

20

EDTA bis-(Methyl tyrosinate): A chelating peptoid peroxynitrite scavenger

Anna E.O. Fisher, Declan P. Naughton

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 132 KB

english, 2003

21

Design and synthesis of novel antihypertensive drugs

P Moutevelis-Minakakis, M Gianni, H Stougiannou, P Zoumpoulakis, A Zoga, A.D Vlahakos, E Iliodromitis, T Mavromoustakos

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 209 KB

english, 2003

22

Facile synthesis of [11C]edrophonium and its analogues as new potential PET imaging agents for heart acetylcholinesterase

Qi-Huang Zheng, Xuan Liu, Xiangshu Fei, Ji-Quan Wang, Bruce H. Mock, Barbara E. Glick-Wilson, Michael L. Sullivan, Gary D. Hutchins

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 150 KB

english, 2003

23

A new sterol sulfate, Sch 572423, from a marine sponge, Topsentia sp.

Shu-Wei Yang, Alexei Buivich, Tze-Ming Chan, Michelle Smith, Jean Lachowicz, Shirley A Pomponi, Amy E Wright, Ronald Mierzwa, Mahesh Patel, Vincent Gullo, Min Chu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 187 KB

english, 2003

24

Substituted bridged phenyl piperidines: orally active growth hormone secretagogues

Zhijian Lu, James R. Tata, Kang Cheng, Liente Wei, Wanda W.-S. Chan, Bridget Butler, Klaus D. Schleim, Thomas M. Jacks, Gerard Hickey, Arthur A. Patchett

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 175 KB

english, 2003

25

Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents

Vedula M. Sharma, K.V. Adi Seshu, C. Vamsee Krishna, P. Prasanna, V. Chandra Sekhar, A. Venkateswarlu, Sriram Rajagopal, R. Ajaykumar, Dhanvanthri S. Deevi, N.V.S. Rao Mamidi, R. Rajagopalan

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 205 KB

english, 2003

26

Inactivation of S-Adenosyl-l-Homocysteine hydrolase with novel 5′-thioadenosine derivatives. Antiviral effects

Georges Guillerm, Danielle Guillerm, Corinne Vandenplas-Vitkowski, Cédric Glapski, Erick De Clercq

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 210 KB

english, 2003

27

A green fluorescent chemosensor for amino acids provides a versatile high-throughput screening (HTS) assay for proteases

Kathryn E.S. Dean, Gérard Klein, Olivier Renaudet, Jean-Louis Reymond

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 167 KB

english, 2003

28

Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors

Manojit Pal, Venugopal Rao Veeramaneni, Murali Nagabelli, Srinivas Rao Kalleda, Parimal Misra, Seshagiri Rao Casturi, Koteswar Rao Yeleswarapu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 171 KB

english, 2003

29

The design of 8,8-Dimethyl[1,6]naphthyridines as potential anticonvulsant agents

Nigel E Austin, Michael S Hadley, John D Harling, Frank P Harrington, Gregor J Macdonald, Darren J Mitchell, Graham J Riley, Tania O Stean, Geoffrey Stemp, Sharon C Stratton, Mervyn Thompson, Neil Upt

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 139 KB

english, 2003

30

Structure–activity relationship on human serum paraoxonase (PON1) using substrate analogues and inhibitors

Rakesh S Bargota, Mahmoud Akhtar, Keith Biggadike, David Gani, Rudolf K Allemann

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 146 KB

english, 2003

31

Study on the mechanism of action of artemether against schistosomes: the identification of cysteine adducts of both carbon-centred free radicals derived from artemether

Wen-Min Wu, Yan-Li Chen, Zili Zhai, Shu-Hua Xiao, Yu-Lin Wu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 134 KB

english, 2003

32

Multidrug resistance reversal activity of key ningalin analogues

Danielle R. Soenen, Inkyu Hwang, Michael P. Hedrick, Dale L. Boger

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 204 KB

english, 2003

33

Synthesis of water-Soluble prodrugs of BMS-191011: A maxi-K channel opener targeted for post-stroke neuroprotection

Piyasena Hewawasam, Min Ding, Nathan Chen, Dalton King, Jay Knipe, Lorraine Pajor, Astrid Ortiz, Valentin K. Gribkoff, John Starrett

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 154 KB

english, 2003

34

Non-imidazole heterocyclic histamine H3 receptor antagonists

Wenying Chai, J.Guy Breitenbucher, Annette Kwok, Xiaobing Li, Victoria Wong, Nicholas I. Carruthers, Timothy W. Lovenberg, Curt Mazur, Sandy J. Wilson, Frank U. Axe, Todd K. Jones

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 165 KB

english, 2003

35

Corrigendum to ‘Design, Synthesis, and Neuraminidase Inhibitory Activity of GS-4071 Analogues that Utilize a Novel Hydrophobic Paradigm’: [Bioorg. Med. Chem. Lett. 12 (2002) 3425]

Stephen Hanessian, Jianchio Wang, Debra Montgomery, Vincent Stoll, Kent D. Stewart, Warren Kati, Clarence Maring, Dale Kempt, Charles Hutchins, W.Graeme Laver

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 77 KB

english, 2003

36

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 54 KB

english, 2003

37

Contents List

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 231 KB

english, 2003

38

Contributors to this Issue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

File:

PDF, 43 KB

2003

39

Graphical Abstracts

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 587 KB

english, 2003

40

Instructions to Contributors and GA example

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 119 KB

english, 2003

41

Discovery of 3-Amino-4-Chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library

Patrick Y.S. Lam, Jessica J. Adams, Charles G. Clark, W.Jason Calhoun, Joseph M. Luettgen, Robert M. Knabb, Ruth R. Wexler

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 216 KB

english, 2003

42

Synthesis, anticholinesterase activity and structure–Activity relationships of m-Aminobenzoic acid derivatives

José Trujillo-Ferrara, Leticia Montoya Cano, Michel Espinoza-Fonseca

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 128 KB

english, 2003

43

Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus

Robert J. Kerns, Michael J. Rybak, Glenn W. Kaatz, Flamur Vaka, Raymond Cha, Richard G. Grucz, Veena U. Diwadkar, Tracey D. Ward

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 167 KB

english, 2003

44

Spiro[pyrrolidine-2,2′-adamantanes]: synthesis, anti-influenza virus activity and conformational properties

Ioannis Stylianakis, Antonios Kolocouris, Nicolas Kolocouris, George Fytas, George B Foscolos, Elizaveta Padalko, Johan Neyts, Erik De Clercq

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 190 KB

english, 2003

45

P-selectin blocking potency of multimeric tyrosine sulfates in vitro and in vivo

Tatyana V Pochechueva, Natalia A Ushakova, Marina E Preobrazhenskaya, Nikolay E Nifantiev, Yu.E Tsvetkov, Marina A Sablina, Alexander B Tuzikov, Mike I Bird, Robert Rieben, Nicolai V Bovin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 145 KB

english, 2003

46

The development of new triazole based inhibitors of tumor necrosis factor-α (TNF-α) production

Joshua S Tullis, John C VanRens, Michael G Natchus, Michael P Clark, Biswanath De, Lily C Hsieh, Michael J Janusz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 160 KB

english, 2003

47

Synthesis of fluorinated 1-(3-Morpholin-4-yl-phenyl)-Ethylamines

Yong-Jin Wu, Huan He, Li-Qiang Sun, Dedong Wu, Qi Gao, Hui-Yin Li

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 173 KB

english, 2003

48

Identification of potent and broad-Spectrum antibiotics from SAR studies of a synthetic vancomycin analogue

Kateri A. Ahrendt, Jacob A. Olsen, Masahiro Wakao, Joaquim Trias, Jonathan A. Ellman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 181 KB

english, 2003

49

5-Aryl thiazolidine-2,4-diones as selective PPARγ agonists

Hiroo Koyama, Julia K Boueres, Wei Han, Edward J Metzger, Jeffrey P Bergman, Dominick F Gratale, Daniel J Miller, Richard L Tolman, Karen L MacNaul, Joel P Berger, Thomas W Doebber, Kwan Leung, David

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 202 KB

english, 2003

50

Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus

Zhijian Lu, Subharekha Raghavan, Joann Bohn, Mark Charest, Mark W. Stahlhut, Carrie A. Rutkowski, Amy L. Simcoe, David B. Olsen, William A. Schleif, Anthony Carella, Lori Gabryelski, Lixia Jin, Jiunn

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 172 KB

english, 2003

51

Design and synthesis of spiro-cyclopentenyl and spiro--dithiolanyl substituted pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease

David M. Andrews, Paul S. Jones, Gail Mills, S.Lucy Hind, Martin J. Slater, Naimisha Trivedi, Katrina J. Wareing

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 164 KB

english, 2003

52

Antibacterial activity of quinolone–Macrocycle conjugates

Elizabeth A. Jefferson, Eric E. Swayze, Stephen A. Osgood, Alycia Miyaji, Lisa M. Risen, Lawrence B. Blyn

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 212 KB

english, 2003

53

Novel synthesis of 2′-O-methylguanosine

Suetying Chow, Ke Wen, Yogesh S. Sanghvi, Emmanuel A. Theodorakis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 141 KB

english, 2003

54

Synthesis and activity of a C-8 keto pleuromutilin derivative

Dane M Springer, Margaret E Sorenson, Stella Huang, Timothy P Connolly, Joanne J Bronson, James A Matson, Ronald L Hanson, David B Brzozowski, Thomas L LaPorte, Ramesh N Patel

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 141 KB

english, 2003

55

Non-Peptide αvβ3 antagonists. Part 6: Design and synthesis of αvβ3 antagonists containing a pyridone or pyrazinone central scaffold

Michael J Breslin, Mark E Duggan, Wasyl Halczenko, Carmen Fernandez-Metzler, Cecilia A Hunt, Chih-Tai Leu, Kara M Merkle, Adel M Naylor-Olsen, Thomayant Prueksaritanont, Gary Stump, Audrey Wallace, Se

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 192 KB

english, 2003

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