Volume 14; Issue 3

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Bioorganic & Medicinal Chemistry Letters
Volume 14; Issue 3

Bioorganic & Medicinal Chemistry Letters

Volume 14; Issue 3

1

Synthesis and SAR evaluation of 1,2,4-triazoles as A2A receptor antagonists

Alexander Alanine, Lilli Anselm, Lucinda Steward, Stefan Thomi, Walter Vifian, Michael D. Groaning

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 218 KB

english, 2004

2

Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: Tertiary amides

Laval Chan, Oswy Pereira, T.Jagadeeswar Reddy, Sanjoy K. Das, Carl Poisson, Marc Courchesne, Mélanie Proulx, Arshad Siddiqui, Constantin G. Yannopoulos, Nghe Nguyen-Ba, Caroline Roy, Daniel Nasturica,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 158 KB

english, 2004

3

Rational design of azepane-glycoside antibiotics targeting the bacterial ribosome

Sofia Barluenga, Klaus B. Simonsen, Ethel S. Littlefield, Benjamin K. Ayida, Dionisios Vourloumis, Geoffrey C. Winters, Masayuki Takahashi, Sarah Shandrick, Qiang Zhao, Qing Han, Thomas Hermann

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 275 KB

english, 2004

4

Synthesis and evaluation of novel bacterial rRNA-binding benzimidazoles by mass spectrometry

Yun He, Jun Yang, Baogen Wu, Dale Robinson, Kelly Sprankle, Pei-Pei Kung, Kristin Lowery, V. Mohan, Steve Hofstadler, Eric E. Swayze, Rich Griffey

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 286 KB

english, 2004

5

Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)

Bin Ye, Yuo-Ling Chou, Rushad Karanjawala, Wheeseong Lee, Shou-Fu Lu, Kenneth J. Shaw, Steven Jones, Dao Lentz, Amy Liang, Jih-Lie Tseng, Qingyu Wu, Zuchun Zhao

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 232 KB

english, 2004

6

Degradation of target protein in living cells by small-molecule proteolysis inducer

Dong Zhang, Sun-Hee Baek, Abby Ho, Kyungbo Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 268 KB

english, 2004

7

Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3

Paola Vianello, Paolo Cozzi, Arturo Galvani, Maurizio Meroni, Mario Varasi, Daniele Volpi, Tiziano Bandiera

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 201 KB

english, 2004

8

QSAR Studies of PC-3 cell line inhibition activity of TSA and SAHA-like hydroxamic acids

Di-Fei Wang, Olaf Wiest, Paul Helquist, Hsuan-Yin Lan-Hargest, Norbert L. Wiech

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 248 KB

english, 2004

9

Inhibition kinetics of carba- and C-fucosyl analogues of GDP-fucose against fucosyltransferase V: implication for the reaction mechanism

Andrew J. Norris, Julian P. Whitelegge, M.Jane Strouse, Kym F. Faull, Tatsushi Toyokuni

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 148 KB

english, 2004

10

3-Trifluoromethyl-4-nitro-5-arylpyrazoles are novel KATP channel agonists

Andrew J. Peat, Claire Townsend, M. Craig McKay, Dulce Garrido, Christopher M. Terry, Jayme L.R. Wilson, Stephen A. Thomson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 210 KB

english, 2004

11

Synthesis of N,N′-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors

Thierry Le Diguarher, Jean-Claude Ortuno, David Shanks, Nicolas Guilbaud, Alain Pierré, Eric Raimbaud, Jean-Luc Fauchère, John A Hickman, Gordon C Tucker, Patrick J Casara

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 251 KB

english, 2004

12

Synthesis and biological results of the technetium-99m-labeled 4-nitroimidazole for imaging tumor hypoxia

Taiwei Chu, Shaowen Hu, Bing Wei, Yi Wang, Xinqi Liu, Xiangyun Wang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 123 KB

english, 2004

13

N-4-Substituted-benzyl-N′-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity

Hyeung-geun Park, Ji-yeon Choi, Sea-hoon Choi, Mi-kyung Park, Jihye Lee, Young-ger Suh, Hawon Cho, Uhtaek Oh, Jiyoun Lee, Sang-Uk Kang, Jeewoo Lee, Hee-Doo Kim, Young-Ho Park, Yeon Su Jeong, Jin Kyu C

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 208 KB

english, 2004

14

Fluorinated dihydroquinolines as potent n-NOS inhibitors

Stefan Jaroch, Hartmut Rehwinkel, Peter Hölscher, Detlev Sülzle, Gerardine Burton, Margrit Hillmann, Fiona M. McDonald, Heribert Miklautz

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 197 KB

english, 2004

15

3D-QSAR studies on PU3 analogues by comparative molecular field analysis

Hong-Chong Liu, Ping-Chiang Lyu, Max K. Leong, Keng-Chang Tsai, Ging-Ho Hsiue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 279 KB

english, 2004

16

Peptidyl aldehydes as slow-binding inhibitors of dual-specificity phosphatases

Junguk Park, Hua Fu, Dehua Pei

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 159 KB

english, 2004

17

A new class of potent non-imidazole H3 antagonists: 2-aminoethylbenzofurans

Marlon Cowart, John K. Pratt, Andrew O. Stewart, Youssef L. Bennani, Timothy A. Esbenshade, Arthur A. Hancock

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 242 KB

english, 2004

18

2-Hydroxy-4-isopropylbenzaldehyde, a potent partial tyrosinase inhibitor

Ken-ichi Nihei, Yoshiro Yamagiwa, Tadao Kamikawa, Isao Kubo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 140 KB

english, 2004

19

Structure–activity relationships of non-imidazole H3 receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists

Gregory A. Gfesser, Henry Zhang, Jurgen Dinges, Gerard B. Fox, Jia Bao Pan, Timothy A. Esbenshade, Betty B. Yao, David Witte, Thomas R. Miller, Chae-Hee Kang, Kathy M. Krueger, Youssef L. Bennani, Art

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 235 KB

english, 2004

20

Synthesis and antifungal activities of phenylenedithioureas

Truong Phuong, Thai Khac-Minh, Nguyen Thi Van Ha, Huynh Thi Ngoc Phuong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 197 KB

english, 2004

21

Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives

C. Yoakim, P.R. Bonneau, R. Déziel, L. Doyon, J. Duan, I. Guse, S. Landry, E. Malenfant, J. Naud, W.W. Ogilvie, J.A. O'Meara, R. Plante, B. Simoneau, B. Thavonekham, M. Bös, M.G. Cordingley

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 167 KB

english, 2004

22

Thiazoles and thiopyridines: novel series of high affinity h5HT7 ligands

Christopher G. Thomson, Margaret S. Beer, Neil R. Curtis, Helen J. Diggle, Emma Handford, Janusz J. Kulagowski

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 190 KB

english, 2004

23

Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

Christopher J Dinsmore, C.Blair Zartman, Jeffrey M Bergman, Marc T Abrams, Carolyn A Buser, J.Christopher Culberson, Joseph P Davide, Michelle Ellis-Hutchings, Christine Fernandes, Samuel L Graham, Ge

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 249 KB

english, 2004

24

Synthesis and antitumor activity of 10-substituted benzylidene anthrone

Weixiao Hu, Wei Zhou

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 146 KB

english, 2004

25

Diamine derivatives with antiparasitic activities

Guillermo R. Labadie, Seoung-Ryoung Choi, Mitchell A. Avery

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 326 KB

english, 2004

26

Biosynthesis of agglomerin A: stereospecific incorporation of pro-R- and pro-S-hydrogens at sn-C-3 of glycerol into the branched C3 moiety

Youichi Mashimo, Yasuyo Sekiyama, Hiroshi Araya, Yoshinori Fujimoto

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 147 KB

english, 2004

27

Synthesis and mitochondrial complex I inhibition of dihydroxy-cohibin A, non-THF annonaceous acetogenin analogue

Hiroyuki Konno, Naoki Hiura, Hidefumi Makabe, Masato Abe, Hideto Miyoshi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 154 KB

english, 2004

28

Permeation and metabolism of a series of novel lipophilic ascorbic acid derivatives, 6-O-acyl-2-O-α-d-glucopyranosyl-l-ascorbic acids with a branched-acyl chain, in a human living skin equivalent model

Akihiro Tai, Satomi Goto, Yutaka Ishiguro, Kazuko Suzuki, Teruhiko Nitoda, Itaru Yamamoto

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 180 KB

english, 2004

29

Synthesis and biological evaluation of novel coumarin derivatives with a 7-azomethine linkage

Christos A. Kontogiorgis, Dimitra J. Hadjipavlou-Litina

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 199 KB

english, 2004

30

Rational design and synthesis of selective BACE-1 inhibitors

Stephen F. Brady, Satendra Singh, Ming-Chih Crouthamel, M.Katharine Holloway, Craig A. Coburn, Victor M. Garsky, Michael Bogusky, Michael W. Pennington, Joseph P. Vacca, Daria Hazuda, Ming-Tain Lai

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 200 KB

english, 2004

31

Aza-bicyclic amino acid sulfonamides as α4β1/α4β7 integrin antagonists

Alexey B Dyatkin, William J Hoekstra, William A Kinney, Maria Kontoyianni, Rosemary J Santulli, Edward S Kimball, M Carolyn Fisher, Stephen M Prouty, William M Abraham, Patricia Andrade-Gordon, Dennis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 265 KB

english, 2004

32

Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics

Yolanda Caro, Marı́a Torrado, Christian F. Masaguer, Enrique Raviña, Fernando Padı́n, José Brea, Marı́a I. Loza

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 203 KB

english, 2004

33

Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid

Chirag K. Patel, Caroline P. Owen, Sabbir Ahmed

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 212 KB

english, 2004

34

Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y5 antagonists

Silvia Galiano, Oihana Erviti, Silvia Pérez, Antonio Moreno, Laura Juanenea, Ignacio Aldana, Antonio Monge

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 146 KB

english, 2004

35

Synthesis and biological evaluation of (−)-laulimalide analogues

Brian M. Gallagher Jr., Francis G. Fang, Charles W. Johannes, Marc Pesant, Martin R. Tremblay, Hongjuan Zhao, Kozo Akasaka, Xiang-yi Li, Junke Liu, Bruce A. Littlefield

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 193 KB

english, 2004

36

Publisher's Announcement—new Regional Editor for Bioorganic & Medicinal Chemistry

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

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english, 2004

37

Editorial Board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 58 KB

english, 2004

38

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 387 KB

english, 2004

39

Contributors to this issue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

File:

PDF, 56 KB

2004

40

Instuctions to Contributors

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 109 KB

english, 2004

41

Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors

Yongxin Han, André Giroux, Erich L. Grimm, Renée Aspiotis, Sébastien Francoeur, Christopher I. Bayly, Daniel J. Mckay, Sophie Roy, Steve Xanthoudakis, John P. Vaillancourt, Dita M. Rasper, John Tam, P

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 312 KB

english, 2004

42

The design and synthesis of sulfonamides as caspase-1 inhibitors

William G. Harter, Hans Albrect, Kenneth Brady, Bradley Caprathe, James Dunbar, John Gilmore, Sheryl Hays, Catherine R. Kostlan, Beth Lunney, Nigel Walker

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 164 KB

english, 2004

43

Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides

Laval Chan, Sanjoy K. Das, T.Jagadeeswar Reddy, Carl Poisson, Mélanie Proulx, Oswy Pereira, Marc Courchesne, Caroline Roy, Wuyi Wang, Arshad Siddiqui, Constantin G. Yannopoulos, Nghe Nguyen-Ba, Denis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 169 KB

english, 2004

44

Synthesis of oligonucleotide 2′-conjugates via amide bond formation in solution

Anna V. Kachalova, Dmitry A. Stetsenko, Michael J. Gait, Tatiana S. Oretskaya

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 181 KB

english, 2004

45

Synthesis and antibiotic activity of the tricyclic furo[3,2-c] isochromen-2-trione unit of the pyranonaphthoquinones

Darı́o A. Bianchi, Emma G. Sutich, Teodoro S. Kaufman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 171 KB

english, 2004

46

Bile acid amides derived from chiral amino alcohols: novel antimicrobials and antifungals

BrajaG. Hazra, VandanaS. Pore, SanjeevKumar Dey, Suchitra Datta, MahendraP. Darokar, Dharmendra Saikia, S.P.S. Khanuja, AnupP. Thakur

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 198 KB

english, 2004

47

Essential structural features of acetogenins: role of hydroxy groups adjacent to the bis-THF rings

Masato Abe, Atsushi Kenmochi, Naoya Ichimaru, Takeshi Hamada, Takaaki Nishioka, Hideto Miyoshi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 159 KB

english, 2004

48

3-(2-Pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT1B/1D ligands

Ian Egle, Neil MacLean, Lidia Demchyshyn, Louise Edwards, Abdelmalik Slassi, Ashok Tehim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 144 KB

english, 2004

49

Design of small molecule ketoamide-based inhibitors of cathepsin K

John G. Catalano, David N. Deaton, Stacey T. Long, Robert B. McFadyen, Larry R. Miller, J.Alan Payne, Kevin J. Wells-Knecht, Lois L. Wright

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 214 KB

english, 2004

50

Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors

Kushol Gupta, Carl J. Kaub, Kristen N. Carey, Eduard G. Casillas, Barry S. Selinsky, Patrick J. Loll

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 225 KB

english, 2004

51

Vancomycin disulfide derivatives as antibacterial agents

YongQi Mu, Matthew Nodwell, John L. Pace, Jeng-Pyng Shaw, J.Kevin Judice

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 203 KB

english, 2004

52

Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent

Uday R. Khire, Donald Bankston, James Barbosa, David R. Brittelli, Yolanda Caringal, Robert Carlson, Jacques Dumas, Todd Gane, Sarah L. Heald, Barbara Hibner, Jeffrey S. Johnson, Michael E. Katz, Nanc

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 178 KB

english, 2004

53

TMC-95A, a reversible proteasome inhibitor, induces neurite outgrowth in PC12 cells

Masayuki Inoue, Haifeng Zhai, Hayato Sakazaki, Hidetomo Furuyama, Yoshiyasu Fukuyama, Masahiro Hirama

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 203 KB

english, 2004

54

Enantioselective ester hydrolysis catalyzed by β-cyclodextrin conjugated with β-hairpin peptides

Hiroshi Tsutsumi, Hiroshi Ikeda, Hisakazu Mihara, Akihiko Ueno

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 177 KB

english, 2004

55

Benzene-di-N-octylcarbamates as conformationally constrained phospholipase A2 inhibitors

Gialih Lin, Yan-Fu Lin, Mei-Ting Hwang, Yu-Zen Lin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 241 KB

english, 2004

56

Inhibition of α-chymotrypsin with thiol-bearing substrate analogues in the presence of zinc ion

Min Su Han, Dong Ju Oh, Dong H. Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 177 KB

english, 2004

57

Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738

Masae Sawada, Ken-ichi Washizuka, Hiroyuki Okumura

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 206 KB

english, 2004

58

Synthesis and incorporation of an α-hexofuranosyl thymidine into oligodeoxynucleotides via its two exocyclic OH-groups

Vyacheslav V. Filichev, Erik B. Pedersen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 178 KB

english, 2004

59

Publisher's Announcement—new Regional Editor for Bioorganic & Medicinal Chemistry

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 62 KB

english, 2004