28 Apr 2008

Bioorganic and Medicinal Chemistry Letters: Vol 18, Issue 8

1.
Editorial board Page IFC

2.
Graphical contents list Pages 2513-2524

3.
Design and campaign synthesis of pyridine-based histone deacetylase inhibitors Pages 2525-2529 David M. Andrews, Keith M. Gibson, Mark A. Graham, Zbigniew S. Matusiak, Craig A. Roberts, Elaine S.E. Stokes, Madeleine C. Brady and Christine M. Chresta

4.
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: Histone deacetylase inhibition and in-cell activities Pages 2530-2535 Antonello Mai, Andrea Perrone, Angela Nebbioso, Dante Rotili, Sergio Valente, Maria Tardugno, Silvio Massa, Floriana De Bellis and Lucia Altucci

5.
Tetrazole based amides as growth hormone secretagogues Pages 2536-2539 James J. Li, Haixia Wang, Jun Li, Fucheng Qu, Stephen G. Swartz, Andrés S. Hernández, Scott A. Biller, Jeffrey A. Robl, Joseph A. Tino, Dorothy Slusarchyk, Ramakrishna Seethala, Paul Sleph, Mujing Yan, Gary Grover, Neil Flynn, Brian J. Murphy and David Gordon

6.
Use of γ-aminopropyl-coated glass surface for the patterning of oligonucleotides through oxime bond formation Pages 2540-2543 Nabil Dendane, Antoine Hoang, Eric Defrancq, Françoise Vinet and Pascal Dumy

7.
Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists Pages 2544-2548 J. Kent Barbay, Yong Gong, Mieke Buntinx, Jian Li, Concha Claes, Pamela J. Hornby, Guy Van Lommen, Jean Van Wauwe and Wei He

8.
Synthesis and biological evaluation of histone deacetylase inhibitors that are based on FR235222: A cyclic tetrapeptide scaffold Pages 2549-2554 Erinprit K. Singh, Suchitra Ravula, Chung-Mao Pan, Po-Shen Pan, Robert C. Vasko, Stephanie A. Lapera, Sujith V.W. Weerasinghe, Mary Kay H. Pflum and Shelli R. McAlpine

9.
Design of high-affinity peptide conjugates with optimized fluorescence quantum yield as markers for small peptide transporter PEPT1 (SLC15A1) Pages 2555-2557 Praveen M. Bahadduri, Abhijit Ray, Akash Khandelwal and Peter W. Swaan

10.
Synthesis and antimicrobial activity of 7α-amino-23,24-bisnor-5α-cholan-22-ol derivatives Pages 2558-2561 Sharaf Nawaz Khan, Young Mee Jung, Bong Jin Kim, Heeyeong Cho, Jinho Lee and Hong-Seok Kim

11.
Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition Pages 2562-2566 Paul V. Fish, Christopher Deur, Xinmin Gan, Keri Greene, David Hoople, Malcolm Mackenny, Kimberly S. Para, Keith Reeves, Thomas Ryckmans, Cory Stiff, Alan Stobie, Florian Wakenhut and Gavin A. Whitlock

12.
Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide–isozyme II adduct Pages 2567-2573 Claudia Temperini, Alessandro Cecchi, Andrea Scozzafava and Claudiu T. Supuran

13.
5-Sulfonyl-benzimidazoles as selective CB2 agonists Pages 2574-2579 Bie M.P. Verbist, Michel A.J. De Cleyn, Michel Surkyn, Erwin Fraiponts, Jeroen Aerssens, Marjoleen J.M.A. Nijsen and Harrie J.M. Gijsen

14.
Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors Pages 2580-2584 David M. Andrews, Elaine S.E. Stokes, Greg R. Carr, Zbigniew S. Matusiak, Craig A. Roberts, Michael J. Waring, Madeleine C. Brady, Christine M. Chresta and Simon J. East

15.
Synthesis and antimicrobial properties of Monensin A esters Pages 2585-2589 Adam Huczyński, Joanna Stefańska, Piotr Przybylski, Bogumil Brzezinski and Franz Bartl

16.
Microarray-based label-free detection of RNA using bispyrene-modified 2′-O-methyl oligoribonucleotide as capture and detection probe Pages 2590-2593 Takashi Sakamoto, Akio Kobori and Akira Murakami

17.
Synthesis of new benzimidazole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates with efficient DNA-binding affinity and potent cytotoxicity Pages 2594-2598 Ahmed Kamal, P. Praveen Kumar, K. Sreekanth, B.N. Seshadri and P. Ramulu

18.
New chemotypes for cathepsin K inhibitors Pages 2599-2603 Naoki Teno, Osamu Irie, Takahiro Miyake, Keigo Gohda, Miyuki Horiuchi, Sachiyo Tada, Kazuhiko Nonomura, Motohiko Kometani, Genji Iwasaki and Claudia Betschart

19.
Exploring predictive QSAR models for hepatocyte toxicity of phenols using QTMS descriptors Pages 2604-2609 Kunal Roy and Paul L.A. Popelier

20.
4′-Methyl-4,5′-bithiazole-based correctors of defective ΔF508-CFTR cellular processing Pages 2610-2614 Choong Leol Yoo, Gui Jun Yu, Baoxue Yang, Lori I. Robins, A.S. Verkman and Mark J. Kurth

21.
Synthesis of 4′-modified noraristeromycins to clarify the effect of the 4′-hydroxyl groups for inhibitory activity against S-adenosyl-l-homocysteine hydrolase Pages 2615-2618 Takayuki Ando, Kenji Kojima, Praveen Chahota, Atsushi Kozaki, Nikalje D. Milind and Yukio Kitade

22.
Hypoxia-inducible factor-1 and nuclear factor-κB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia Pages 2619-2623 Cheng-Zhu Wu, Seong Su Hong, Xing Fu Cai, Nguyen Tien Dat, Ji-Xing Nan, Bang Yeon Hwang, Jung Joon Lee and Dongho Lee

23.
Selective vasodilatation effect of sargahydroquinoic acid, an active constituent of Sargassum micracanthum, on the basilar arteries of rabbits Pages 2624-2627 Byong-Gon Park, Woon-Seob Shin, Yumi Um, Sungsik Cho, Gab-Man Park, Dong-Soo Yeon, Seong-Chun Kwon, Jungyeob Ham, Byoung Wook Choi and Seokjoon Lee

24.
Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds Pages 2628-2632 Joshua Roth, Franck Madoux, Peter Hodder and William R. Roush

25.
Structure-dependent inhibition of bladder and pancreatic cancer cell growth by 2-substituted glycyrrhetinic and ursolic acid derivatives Pages 2633-2639 Gayathri Chadalapaka, Indira Jutooru, Alan McAlees, Tom Stefanac and Stephen Safe

26.
2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: Optimization via array synthesis Pages 2640-2644 Lalgudi S. Harikrishnan, Muthoni G. Kamau, Timothy F. Herpin, George C. Morton, Yalei Liu, Christopher B. Cooper, Mark E. Salvati, Jennifer X. Qiao, Tammy C. Wang, Leonard P. Adam, David S. Taylor, Alice Ye A. Chen, Xiaohong Yin, Ramakrishna Seethala, Tara L. Peterson, David S. Nirschl, Arthur V. Miller, Carolyn A. Weigelt, Kingsley K. Appiah, Jonathan C. O’Connell and R. Michael Lawrence

27.
Novel antibacterial azetidine lincosamides Pages 2645-2648 Hardwin O’Dowd, Jason G. Lewis, Joaquim Trias, Rumi Asano, Johanne Blais, Sara L. Lopez, Craig K. Park, Charlotte Wu, Wen Wang and Mikhail F. Gordeev

28.
N-d-Aldopentofuranosyl-N′-[p-(isoamyloxy)phenyl]-thiourea derivatives: Potential anti-TB therapeutic agents Pages 2649-2651 Avraham Liav, Shiva K. Angala, Patrick J. Brennan and Mary Jackson

29.
Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38α inhibitors Pages 2652-2657 Jagabandhu Das, Robert V. Moquin, Sidney Pitt, Rosemary Zhang, Ding Ren Shen, Kim W. McIntyre, Kathleen Gillooly, Arthur M. Doweyko, John S. Sack, Hongjian Zhang, Susan E. Kiefer, Kevin Kish, Murray McKinnon, Joel C. Barrish, John H. Dodd, Gary L. Schieven and Katerina Leftheris

30.
Novel bisbenzimidazoles with antileishmanial effectiveness Pages 2658-2661 Annie Mayence, Aurélie Pietka, Margaret S. Collins, Melanie T. Cushion, Babu L. Tekwani, Tien L. Huang and Jean Jacques Vanden Eynde

31.
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis Pages 2662-2668 Karen L. Stirrett, Julian A. Ferreras, Venkatesan Jayaprakash, Barij N. Sinha, Tao Ren and Luis E.N. Quadri

32.
Carbonic anhydrase inhibitors: The X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors Pages 2669-2674 Anna Di Fiore, Carlo Pedone, Jochen Antel, Harald Waldeck, Andreas Witte, Michael Wurl, Andrea Scozzafava, Claudiu T. Supuran and Giuseppina De Simone

33.
Alkyne–quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD Pages 2675-2678 Jean-Philippe Starck, Laurent Provins, Bernard Christophe, Michel Gillard, Sophie Jadot, Patrick Lo Brutto, Luc Quéré, Patrice Talaga and Michel Guyaux

34.
A novel bifunctional maleimido CHX-A″ chelator for conjugation to thiol-containing biomolecules Pages 2679-2683 Heng Xu, Kwamena E. Baidoo, Karen J. Wong and Martin W. Brechbiel

35.
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping Pages 2684-2690 Adrian Hall, Andy Billinton, Susan H. Brown, Anita Chowdhury, Gerard M.P. Giblin, Paul Goldsmith, David N. Hurst, Alan Naylor, Sadhana Patel, Tiziana Scoccitti and Pamela J. Theobald

36.
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors Pages 2691-2695 Vijaya Gracias, Zhiqin Ji, Irini Akritopoulou-Zanze, Cele Abad-Zapatero, Jeffrey R. Huth, Danying Song, Philip J. Hajduk, Eric F. Johnson, Keith B. Glaser, Patrick A. Marcotte, Lori Pease, Nirupama B. Soni, Kent D. Stewart, Steven K. Davidsen, Michael R. Michaelides and Stevan W. Djuric

37.
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold Pages 2696-2700 Christian Beaulieu, Daniel Guay, Zhaoyin Wang, Yves Leblanc, Patrick Roy, Claude Dufresne, Robert Zamboni, Carl Berthelette, Stephen Day, Nancy Tsou, Danielle Denis, Gillian Greig, Marie-Claude Mathieu and Gary O’Neill

38.
A molecular modeling study of the interaction of 2′-fluoro-substituted analogues of dUMP/FdUMP with thymidylate synthase Pages 2701-2708 Adam Jarmuła, Anna Dowierciał and Wojciech Rode

39.
Development of 2-tbutyl-N-methyl pyrimidones as potent inhibitors of HIV integrase Pages 2709-2713 M. Emilia Di Francesco, Paola Pace, Fabrizio Fiore, Francesca Naimo, Fabio Bonelli, Michael Rowley and Vincenzo Summa

40.
Pyrano-[2,3b]-pyridines as potassium channel antagonists Pages 2714-2718 Heather J. Finlay, John Lloyd, Michael Nyman, Mary Lee Conder, Tonya West, Paul Levesque and Karnail Atwal

41.
PTP1B inhibitors: Synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold Pages 2719-2724 Christopher P. Holmes, Xianfeng Li, Yijun Pan, Caiding Xu, Ashok Bhandari, Claire M. Moody, Joy A. Miguel, Steven W. Ferla, M. Nuria De Francisco, Brian T. Frederick, Siqun Zhou, Natalie Macher, Larry Jang, Jennifer D. Irvine and J. Russell Grove

42.
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists Pages 2725-2729 Thomas J. Woltering, Jürgen Wichmann, Erwin Goetschi, Geo Adam, James N.C. Kew, Frédéric Knoflach, Theresa M. Ballard, Jörg Huwyler, Vincent Mutel and Silvia Gatti

43.
N-Pyridin-3-yl- and N-quinolin-3-yl-benzamides: Modulators of Human Vanilloid Receptor 1 (TRPV1) Pages 2730-2734 Michele C. Jetter, James J. McNally, Mark A. Youngman, Mark E. McDonnell, Adrienne E. Dubin, Nadia Nasser, Sui-Po Zhang, Ellen E. Codd, Ray W. Colburn, Dennis R. Stone, Michael R. Brandt, Christopher M. Flores and Scott L. Dax

44.
Des-A-ring benzothiadiazines: Inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerase Pages 2735-2738 Pamela L. Donner, Qinghua Xie, John K. Pratt, Clarence J. Maring, Warren Kati, Wen Jiang, Yaya Liu, Gennadiy Koev, Sherie Masse, Debra Montgomery, Akhter Molla and Dale J. Kempf

45.
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38α MAP kinase inhibitors Pages 2739-2744 Stephen T. Wrobleski, Shuqun Lin, John Hynes Jr., Hong Wu, Sidney Pitt, Ding Ren Shen, Rosemary Zhang, Kathleen M. Gillooly, David J. Shuster, Kim W. McIntyre, Arthur M. Doweyko, Kevin F. Kish, Jeffrey A. Tredup, Gerald J. Duke, John S. Sack, Murray McKinnon, John Dodd, Joel C. Barrish, Gary L. Schieven and Katerina Leftheris

46.
Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor Pages 2745-2750 John T. Randolph, Xiaolin Zhang, Peggy P. Huang, Larry L. Klein, Kevin A. Kurtz, Alex K. Konstantinidis, Wenping He, Warren M. Kati and Dale J. Kempf

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