Volume 13; Issue 19

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Bioorganic & Medicinal Chemistry Letters
Volume 13; Issue 19

Bioorganic & Medicinal Chemistry Letters

Volume 13; Issue 19

1

Synthesis of pyrimidinopyridine–triazene conjugates targeted to abl tyrosine kinase

Zakaria Rachid, Athanasia Katsoulas, Fouad Brahimi, Bertrand Jacques Jean-Claude

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 169 KB

english, 2003

2

Detection of 1270 nm emission from singlet oxygen and photocytotoxic property of sugar-Pendant [60] fullerenes

Yuji Mikata, Satowa Takagi, Maki Tanahashi, Sayoko Ishii, Makoto Obata, Yuichi Miyamoto, Kazuhito Wakita, Tsuyoshi Nishisaka, Toru Hirano, Toshiaki Ito, Mikio Hoshino, Chikara Ohtsuki, Masao Tanihara,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 217 KB

english, 2003

3

N1-Benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates

Manik R. Pullagurla, Małgorzata Dukat, Vincent Setola, Bryan Roth, Richard A. Glennon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 193 KB

english, 2003

4

Synthesis and Structure–activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor

Fabio C. Tucci, Yun-Fei Zhu, Zhiqiang Guo, Timothy D. Gross, Patrick J. Connors Jr., R.Scott Struthers, Greg J. Reinhart, John Saunders, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 214 KB

english, 2003

5

Synthesis and Structure–Activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists

Zhiqiang Guo, Yun-Fei Zhu, Fabio C. Tucci, Yinghong Gao, R.Scott Struthers, John Saunders, Timothy D. Gross, Qiu Xie, Greg J. Reinhart, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 192 KB

english, 2003

6

Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-Releasing factor receptor type-1 antagonists

Keith Wilcoxen, Charles Q Huang, James R McCarthy, Dimitri E Grigoriadis, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 180 KB

english, 2003

7

Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists

Charles Q. Huang, Keith Wilcoxen, James R. McCarthy, Mustaph Haddach, Dimitri Grigoriadis, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 153 KB

english, 2003

8

Glycidol-carbohydrate hybrids: a new family of DNA alkylating agents

Kazunobu Toshima, Yukiko Okuno, Shuichi Matsumura

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 174 KB

english, 2003

9

Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression

Lorraine Axford, John R. Boot, Terrence M. Hotten, Martine Keenan, Fionna M. Martin, Sandra Milutinovic, Nick A. Moore, Michael F. O'Neill, Ian A. Pullar, David E. Tupper, Kristel R. Van Belle, Vincen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 177 KB

english, 2003

10

2-Piperidin-4-yl-benzimidazoles with broad spectrum antibacterial activities

Yun He, Baogen Wu, Jun Yang, Dale Robinson, Lisa Risen, Ray Ranken, Lawrence Blyn, Suzie Sheng, Eric E Swayze

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 179 KB

english, 2003

11

Electrostatic interaction of π-Acidic amides with hydrogen-Bond acceptors

Yi Li, Lawrence B. Snyder, David R. Langley

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 333 KB

english, 2003

12

Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase

Sergio H. Szajnman, Andrea Montalvetti, Youhong Wang, Roberto Docampo, Juan B. Rodriguez

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 200 KB

english, 2003

13

Cyclohexanedione herbicides are inhibitors of rat heart acetyl-CoA carboxylase

Thomas W Seng, Tiffanie R Skillman, Nengyu Yang, Craig Hammond

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 231 KB

english, 2003

14

Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor

Zhengming Chen, Wendy S Miller, Shen Shan, Kenneth J Valenzano

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 220 KB

english, 2003

15

Synthesis and biological activity of piperazine-Based dual MMP-13 and TNF-α converting enzyme inhibitors

Michael A. Letavic, John T. Barberia, Thomas J. Carty, Joel R. Hardink, Jennifer Liras, Lori L. Lopresti-Morrow, Peter G. Mitchell, Mark C. Noe, Lisa M. Reeves, Sheri L. Snow, Ethan J. Stam, Francis J

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 172 KB

english, 2003

16

Synthesis of methyl (5S,6R,7E,9E,11Z,13E,15S)-16-(4-fluorophenoxy)-5,6,15-trihydroxy-7,9,11,13-hexadecatetraenoate, an analogue of 15R-Lipoxin A4

Eifion D Phillips, Hui-Fang Chang, Christopher R Holmquist, John P McCauley

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 155 KB

english, 2003

17

Xylylated dimers of putrescine and polyamines: influence of the polyamine backbone on spermidine transport inhibition

Laurence Covassin, Michel Desjardins, Denis Soulet, René Charest-Gaudreault, Marie Audette, Richard Poulin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 158 KB

english, 2003

18

Synthesis of a novel family of diterpenes and their evaluation as anti-inflammatory agents

Thanh Lam, Taotao Ling, Chinmay Chowdhury, Ta-Hsiang Chao, F.R. Bahjat, G.K. Lloyd, Lyle L. Moldawer, Michael A. Palladino, Emmanuel A. Theodorakis

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 287 KB

english, 2003

19

Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase

T.Jagadeeswar Reddy, Laval Chan, Nathalie Turcotte, Melanie Proulx, Oswy Z. Pereira, Sanjoy K. Das, Arshad Siddiqui, Wuyi Wang, Carl Poisson, Constantin G. Yannopoulos, Darius Bilimoria, Lucille L'Heu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 147 KB

english, 2003

20

Muraymycins, novel peptidoglycan biosynthesis inhibitors: synthesis and SAR of their analogues

Ayako Yamashita, Emily Norton, Peter J Petersen, Beth A Rasmussen, Guy Singh, Youjin Yang, Tarek S Mansour, Douglas M Ho

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 274 KB

english, 2003

21

Stereoselective synthesis of phosphoramidate α(2-6)Sialyltransferase transition-State analogue inhibitors

Danielle Skropeta, Ralf Schwörer, Richard R. Schmidt

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 165 KB

english, 2003

22

Novel inhibitors of an emerging target in Mycobacterium tuberculosis; substituted thiazolidinones as inhibitors of dTDP-rhamnose synthesis

Kerim Babaoglu, Mark A. Page, Victoria C. Jones, Michael R. McNeil, Changjiang Dong, James H. Naismith, Richard E. Lee

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 228 KB

english, 2003

23

A convenient method for the computer-Aided molecular design of carborane containing compounds

Jayaseharan Johnsamuel, Youngjoo Byun, Thomas P. Jones, Yasuyuki Endo, Werner Tjarks

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 200 KB

english, 2003

24

Synthesis and PDF inhibitory activities of novel benzothiazolylidenehydroxamic acid derivatives

Wataru Takayama, Yoshihisa Shirasaki, Yusuke Sakai, Emi Nakajima, Shuhei Fujita, Kanako Sakamoto-Mizutani, Jun Inoue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 206 KB

english, 2003

25

Structure of Plasmodium vivax dihydrofolate reductase determined by homology modeling and molecular dynamics refinement

Giulio Rastelli, Sara Pacchioni, Marco Daniele Parenti

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 415 KB

english, 2003

26

Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid

Jürgen Einsiedel, Klaus Weber, Christoph Thomas, Thomas Lehmann, Harald Hübner, Peter Gmeiner

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 216 KB

english, 2003

27

Design and synthesis of dimeric HIV-1 integrase inhibitory peptides

Krzysztof Krajewski, Ya-Qiu Long, Christophe Marchand, Yves Pommier, Peter P. Roller

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 139 KB

english, 2003

28

HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1′ substituent

Joseph L. Duffy, Brian A. Kirk, Nancy J. Kevin, Kevin T. Chapman, William A. Schleif, David B. Olsen, Mark Stahlhut, Carrie A. Rutkowski, Lawrence C. Kuo, Lixia Jin, Jiunn H. Lin, Emilio A. Emini, Jam

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 178 KB

english, 2003

29

Activity predictions for efavirenz analogues with the K103N mutant of HIV reverse transcriptase

Marina Udier-Blagović, Edward K. Watkins, Julian Tirado-Rives, William L. Jorgensen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 200 KB

english, 2003

30

Synthetic dihydropacidamycin antibiotics: A modified spectrum of activity for the pacidamycin class

Constantine G. Boojamra, Rémy C. Lemoine, Johanne Blais, Nicole G. Vernier, Karin A. Stein, Angela Magon, Suzanne Chamberland, Scott J. Hecker, Ving J. Lee

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 167 KB

english, 2003

31

Structure activity studies of a novel cytotoxic benzodiazepine

Anthony Boitano, Cory D Emal, Francesco Leonetti, Neal B Blatt, Thomas A Dineen, Jonathan A Ellman, William R Roush, Anthony W Opipari, Gary D Glick

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 163 KB

english, 2003

32

Synthesis and SAR of 8-Arylquinolines as potent corticotropin-Releasing factor1 (CRF1) receptor antagonists

Charles Q. Huang, Keith Wilcoxen, James R. McCarthy, Mustapha Haddach, Thomas R. Webb, Jian Gu, Yun-Feng Xie, Dimitri E. Grigoriadis, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 187 KB

english, 2003

33

α-Keto amides as inhibitors of histone deacetylase

Carol K. Wada, Robin R. Frey, Zhiqin Ji, Michael L. Curtin, Robert B. Garland, James H. Holms, Junling Li, Lori J. Pease, Jun Guo, Keith B. Glaser, Patrick A. Marcotte, Paul L. Richardson, Shannon S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 258 KB

english, 2003

34

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

Bin Ye, Shawn Bauer, Brad O. Buckman, Ameen Ghannam, Brian D. Griedel, Seock-Kyu Khim, Wheeseong Lee, Karna L. Sacchi, Kenneth J. Shaw, Amy Liang, Qingyu Wu, Zuchun Zhao

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 212 KB

english, 2003

35

Synthesis and anthelmintic activity of cyclohexadepsipeptides with (S,S,S,R,S,R)-configuration

Peter Jeschke, Jordi Benet-Buchholz, Achim Harder, Winfried Etzel, Michael Schindler, Gerhard Thielking

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 249 KB

english, 2003

36

The stability of pseudopeptides bearing sulfoximines as chiral backbone modifying element towards proteinase K

Carsten Bolm, Dirk Müller, Christian Dalhoff, Christian P.R. Hackenberger, Elmar Weinhold

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 176 KB

english, 2003

37

O-Arylmandelic acids as highly selective human PPAR α/γ agonists

Alan D Adams, Zao Hu, Derek von Langen, Adonis Dadiz, Alex Elbrecht, Karen L MacNaul, Joel P Berger, Gaochao Zhou, Thomas W Doebber, Roger Meurer, Michael J Forrest, David E Moller, A Brian Jones

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 212 KB

english, 2003

38

Design and synthesis of fluorinated RXR modulators

D.L. Gernert, R. Ajamie, R.A. Ardecky, M.G. Bell, M.D. Leibowitz, D.A. Mais, C.M. Mapes, P.Y. Michellys, D. Rungta, A. Reifel-Miller, J.S. Tyhonas, N. Yumibe, T.A. Grese

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 188 KB

english, 2003

39

Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands

Marı́a L. López-Rodrı́guez, Bellinda Benhamú, Mª José Morcillo, Ignacio Tejada, David Avila, Isabel Marco, Lucio Schiapparelli, Diana Frechilla, Joaquı́n Del Rı́o

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 153 KB

english, 2003

40

Regulation of gene expression by synthetic dimerizers with novel specificity

Wu Yang, Terence P. Keenan, Leonard W. Rozamus, Xiurong Wang, Victor M. Rivera, Carl T. Rollins, Tim Clackson, Dennis A. Holt

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 156 KB

english, 2003

41

Antiallergic principles from Alpinia galanga: structural requirements of phenylpropanoids for inhibition of degranulation and release of TNF-α and IL-4 in RBL-2H3 cells

Hisashi Matsuda, Toshio Morikawa, Hiromi Managi, Masayuki Yoshikawa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 197 KB

english, 2003

42

De novo synthesis of two new cytotoxic tiazofurin analogues with modified sugar moieties

Mirjana Popsavin, Ljilja Torović, Vesna Kojić, Gordana Bogdanović, Saša Spaić, Velimir Popsavin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 153 KB

english, 2003

43

1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists

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

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 218 KB

english, 2003

44

Analysis of the Critical Structural Determinant(s) of Species-Selective Peroxisome Proliferator-Activated Receptor Alpha (PPARα)-Activation by Phenylpropanoic Acid-Type PPARα Agonists

Hiroyuki Miyachi, Hideharu Uchiki

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 207 KB

english, 2003

45

Synthesis of S6-(2,4-dinitrophenyl)-6-thioguanosine phosphoramidite and its incorporation into oligoribonucleotides

Qinguo Zheng, Yang Wang, Eric Lattmann

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 144 KB

english, 2003

46

Selective 3-Amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-Arginine mimetics

Lucija Peterlin-Mašič, Andreja Kranjc, Petra Marinko, Gregor Mlinšek, Tomaž Šolmajer, Mojca Stegnar, Danijel Kikelj

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 280 KB

english, 2003

47

Biological activities of α-mangostin derivatives against acidic sphingomyelinase

Motoko Hamada, Kazuhiko Iikubo, Yuichi Ishikawa, Aya Ikeda, Kazuo Umezawa, Shigeru Nishiyama

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 136 KB

english, 2003

48

Reversed hydroxamate-Bearing thermolysin inhibitors mimic a high-energy intermediate along the enzyme-Catalyzed proteolytic reaction pathway

Jung Dae Park, Dong H Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 185 KB

english, 2003

49

Arachidonylsulfonyl derivatives as cannabinoid CB1 receptor and fatty acid amide hydrolase inhibitors

Yoffi Segall, Gary B. Quistad, Daniel K. Nomura, John E. Casida

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 132 KB

english, 2003

50

Synthesis and cytotoxic activity of a-ring modified betulinic acid derivatives

Young-Jae You, Yong Kim, Nguyen-Hai Nam, Byung-Zun Ahn

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 176 KB

english, 2003

51

Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors

Zhonghua Pei, Xiaofeng Li, Gang Liu, Cele Abad-Zapatero, Tom Lubben, Tianyuan Zhang, Stephen J. Ballaron, Charles W. Hutchins, James M. Trevillyan, Michael R. Jirousek

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 211 KB

english, 2003

52

Synthesis and SAR evaluation of oxadiazolopyrazines as selective Haemophilus influenzae antibacterial agents

Xenia Beebe, Angela M. Nilius, Philip J. Merta, Niru B. Soni, Mai H. Bui, Rolf Wagner, Bruce A. Beutel

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 157 KB

english, 2003

53

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 58 KB

english, 2003

54

Contents List

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 119 KB

english, 2003

55

Contributors to this Issue

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

File:

PDF, 50 KB

2003

56

Graphical Abstracts

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 359 KB

english, 2003

57

Instructions to Contributors and GA example

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 119 KB

english, 2003

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