7 Mar 2008

Bioorganic and Medicinal Chemistry Letters: Vol 18, Issue 5

Individual stereoisomers of phosphinic dipeptide inhibitor of leucine aminopeptidasePages 1550-1554Artur Mucha, Michael Lämmerhofer, Wolfgang Lindner, Małgorzata Pawełczak and Paweł Kafarski
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4.
Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277Pages 1555-1558Lin Zhou, André Alker, Armin Ruf, Xiaofang Wang, Francis C.K. Chiu, Julia Morizzi, Susan A. Charman, William N. Charman, Christian Scheurer, Sergio Wittlin, Yuxiang Dong, Daniel Hunziker and Jonathan L. Vennerstrom
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5.
New cytotoxic saturated and unsaturated cyclohexanones from Anthemis maritimaPages 1559-1562Francesca Collu, Leonardo Bonsignore, Mariano Casu, Costantino Floris, Jürg Gertsch and Filippo Cottiglia
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6.
6-Acetyl-7,7-dimethyl-5,6,7,8-tetrahydropterin is an activator of nitric oxide synthasesPages 1563-1566Colin J. Suckling, Colin L. Gibson, Judith K. Huggan, Raghavendar R. Morthala, Brendan Clarke, Suma Kununthur, Roger M. Wadsworth, Simon Daff and Davide Papale
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7.
Pyrogallol and its analogs can antagonize bacterial quorum sensing in Vibrio harveyiPages 1567-1572Nanting Ni, Gaurav Choudhary, Minyong Li and Binghe Wang
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8.
Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3Pages 1573-1576Martin E. Hayes, Grier A. Wallace, Pintipa Grongsaard, Agnieszka Bischoff, Dawn M. George, Wenyan Miao, Michael J. McPherson, Robert H. Stoffel, David W. Green and Gregory P. Roth
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9.
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-α Converting Enzyme (TACE): Novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1′ substituentsPages 1577-1582Gregory R. Ott, Naoyuki Asakawa, Zhonghui Lu, Rajan Anand, Rui-Qin Liu, Maryanne B. Covington, Krishna Vaddi, Mingxin Qian, Robert C. Newton, David D. Christ, James M. Trzaskos and James J.-W. Duan
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10.
Carbonic anhydrase inhibitors: Interactions of phenols with the 12 catalytically active mammalian isoforms (CA I–XIV)Pages 1583-1587Alessio Innocenti, Daniela Vullo, Andrea Scozzafava and Claudiu T. Supuran
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11.
Conformational significance of EH21A1–A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activityPages 1588-1591Hideyuki Onodera, Masami Kaneko, Yuichi Takahashi, Yumiko Uochi, Jun Funahashi, Takayuki Nakashima, Shiro Soga, Makoto Suzuki, Shunichi Ikeda, Yoshinori Yamashita, Endang S. Rahayu, Yutaka Kanda and Michio Ichimura
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12.
Novel methylene-linked heterocyclic EP1 receptor antagonistsPages 1592-1597Adrian Hall, Rino A. Bit, Susan H. Brown, Anita Chowdhury, Gerard M.P. Giblin, David N. Hurst, Ian R. Kilford, Xiao Lewell, Alan Naylor and Tiziana Scoccitti
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13.
Use of the X-ray structure of the Beta2-adrenergic receptor for drug discoveryPages 1598-1602Sid Topiol and Michael Sabio
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14.
Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1sPages 1603-1606Jeremy M. Travins, Farah Ali, Hui Huang, Shelley K. Ballentine, Ehab Khalil, Heather R. Hufnagel, Wenxi Pan, Joan Gushue, Kristi Leonard, Roger F. Bone, Richard M. Soll, Renee L. DesJarlais, Carl S. Crysler, Nisha Ninan, Jennifer Kirkpatrick, Maxwell D. Cummings, Norman Huebert, Christopher J. Molloy, Michael Gaul, Bruce E. Tomczuk, et al.
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15.
Design, synthesis, and evaluation of novel ethambutol analoguesPages 1607-1611Raghunandan Yendapally and Richard E. Lee
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16.
Structure–activity relationships of 2-chloro-N6-substituted-4′-thioadenosine-5′-N,N-dialkyluronamides as human A3 adenosine receptor antagonistsPages 1612-1616Lak Shin Jeong, Hyuk Woo Lee, Hea Ok Kim, Dilip K. Tosh, Shantanu Pal, Won Jun Choi, Zhan-Guo Gao, Amit R. Patel, Wanda Williams, Kenneth A. Jacobson and Hee-Doo Kim
Abstract Full Text + Links PDF (142 K)
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17.
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARα/γ agonists. Part I: Synthesis and pharmacological evaluationPages 1617-1622Cécile Parmenon, Jérôme Guillard, Daniel-Henri Caignard, Nathalie Hennuyer, Bart Staels, Valérie Audinot-Bouchez, Jean-Albert Boutin, Catherine Dacquet, Alain Ktorza and Marie-Claude Viaud-Massuard
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18.
Aurora kinase A inhibitors: Identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffoldPages 1623-1627Mohane Selvaraj Coumar, Jian-Sung Wu, Jiun-Shyang Leou, Uan-Kang Tan, Chung-Yu Chang, Teng-Yuan Chang, Wen-Hsing Lin, John T.-A. Hsu, Yu-Sheng Chao, Su-Ying Wu and Hsing-Pang Hsieh
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19.
Isoindol-1,3-dione and isoindol-1-one derivatives with high binding affinity to β-amyloid fibrilsPages 1628-1631Hyu Ji Lee, Soo Jeong Lim, Seung Jun Oh, Dae Hyuk Moon, Dong Jin Kim, Jinsung Tae and Kyung Ho Yoo
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20.
A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapyPages 1632-1636Yoshiyuki Yoneda, Sebastian C.J. Steiniger, Kateřina Čapková, Jenny M. Mee, Ying Liu, Gunnar F. Kaufmann and Kim D. Janda
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21.
Synthesis of hybrid acetogenins, α,β-unsaturated-γ-lactone-free nitrogen-containing heterocyclic analogues, and their cytotoxicity against human cancer cell linesPages 1637-1641Naoto Kojima, Tetsuya Fushimi, Naoyoshi Maezaki, Tetsuaki Tanaka and Takao Yamori
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22.
Discovery of novel FMS kinase inhibitors as anti-inflammatory agentsPages 1642-1648Carl R. Illig, Jinsheng Chen, Mark J. Wall, Kenneth J. Wilson, Shelley K. Ballentine, M. Jonathan Rudolph, Renee L. DesJarlais, Yanmin Chen, Carsten Schubert, Ioanna Petrounia, Carl S. Crysler, Christopher J. Molloy, Margery A. Chaikin, Carl L. Manthey, Mark R. Player, Bruce E. Tomczuk and Sanath K. Meegalla
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23.
BACE1 inhibitors: Optimization by replacing the residue with non-acidic moietyPages 1649-1653Yoshio Hamada, Hamdy Abdel-Rahman, Abdellah Yamani, Jeffrey-Tri Nguyen, Monika Stochaj, Koushi Hidaka, Tooru Kimura, Yoshio Hayashi, Kazuki Saito, Shoichi Ishiura and Yoshiaki Kiso
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24.
Novel non-peptidic and small-sized BACE1 inhibitorsPages 1654-1658Yoshio Hamada, Hiroko Ohta, Naoko Miyamoto, Ryoji Yamaguchi, Abdellah Yamani, Koushi Hidaka, Tooru Kimura, Kazuki Saito, Yoshio Hayashi, Shoichi Ishiura and Yoshiaki Kiso
Abstract Full Text + Links PDF (924 K)
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25.
Synthesis and biological evaluation of novel 8-aminomethylated oroxylin A analogues as α-glucosidase inhibitorsPages 1659-1662T. Hari Babu, V. Rama Subba Rao, Ashok K. Tiwari, K. Suresh Babu, P.V. Srinivas, Amtul Z. Ali and J. Madhusudana Rao
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26.
Synthesis and antioxidant activities of 3,5-dialkoxy-4-hydroxycinnamamidesPages 1663-1667Tae-Souk Kang, Hyang-Ok Jo, Woo-Kyu Park, Jong-Pyung Kim, Yasuo Konishi, Jae-Yang Kong, No-Sang Park and Young-Sik Jung
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27.
Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligandsPages 1668-1673Francisco Cuenca, Olga Greciano, Mekala Gunaratnam, Shozeb Haider, Deeksha Munnur, Rupesh Nanjunda, W. David Wilson and Stephen Neidle
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28.
In vitro and in vivo evaluation of O-alkyl derivatives of tramadolPages 1674-1680Liming Shao, Michael Hewitt, Thomas P. Jerussi, Frank Wu, Scott Malcolm, Paul Grover, Kevin Fang, Patrick Koch, Chris Senanayake, Nandkumar Bhongle, Seth Ribe, Roger Bakale and Mark Currie
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29.
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1′ modifications for the exploration of the S1′ subsitePages 1681-1687David N. Deaton, Kevin P. Graham, Jeffrey W. Gross and Aaron B. Miller
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30.
Constraining the amide bond in N-Sulfonylated dipeptide VLA-4 antagonistsPages 1688-1691Linda L. Chang, Ginger X. Yang, Ermengilda McCauley, Richard A. Mumford, John A. Schmidt and William K. Hagmann
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31.
Synthesis of potent pyrrolidine influenza neuraminidase inhibitorsPages 1692-1695A. Chris Krueger, Yibo Xu, Warren M. Kati, Dale J. Kempf, Clarence J. Maring, Keith F. McDaniel, Akhteruzzaman Molla, Debra Montgomery and William E. Kohlbrenner
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32.
Imidazopyridines: A novel class of hNav1.7 channel blockersPages 1696-1701Clare London, Scott B. Hoyt, William H. Parsons, Brande S. Williams, Vivien A. Warren, Richard Tschirret-Guth, McHardy M. Smith, Birgit T. Priest, Erin McGowan, William J. Martin, Kathryn A. Lyons, Xiaohua Li, Bindhu V. Karanam, Nina Jochnowitz, Maria L. Garcia, John P. Felix, Brian Dean, Catherine Abbadie, Gregory J. Kaczorowski and Joseph L. Duffy
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33.
2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924Pages 1702-1707Mark G. Saulnier, David B. Frennesson, Mark D. Wittman, Kurt Zimmermann, Upender Velaparthi, David R. Langley, Charles Struzynski, Xiaopeng Sang, Joan Carboni, Aixin Li, Ann Greer, Zheng Yang, Praveen Balimane, Marco Gottardis, Ricardo Attar and Dolatrai Vyas
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34.
Thiosemicarbazones active against Clostridium difficilePages 1708-1711Cait Costello, Tarja Karpanen, Peter A. Lambert, Preena Mistry, Katy J. Parker, Daniel L. Rathbone, Jiangmeng Ren, Laura Wheeldon and Tony Worthington
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35.
Transkarbams with terminal branching as transdermal permeation enhancersPages 1712-1715Jana Klimentová, Petr Kosák, Kateřina Vávrová, Tomáš Holas, Jakub Novotný and Alexandr Hrabálek
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36.
A potential new prodrug for the treatment of cystinosis: Design, synthesis and in-vitro evaluationPages 1716-1719Bridgeen McCaughan, Graeme Kay, Rachel M. Knott and Donald Cairns
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37.
An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activityPages 1720-1724Gemma L. Ellis, Richard Amewu, Charlotte Hall, Karen Rimmer, Steven A. Ward and Paul M. O’Neill
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38.
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivityPages 1725-1729Monika Ermann, Doris Riether, Edward R. Walker, Innocent F. Mushi, James E. Jenkins, Beatriz Noya-Marino, Mark L. Brewer, Malcolm G. Taylor, Patricia Amouzegh, Stephen P. East, Brian W. Dymock, Mark J. Gemkow, Andreas F. Kahrs, Andreas Ebneth, Sabine Löbbe, Kathy O’Shea, Daw-Tsun Shih and David Thomson
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39.
2-Aminotetralones: Novel inhibitors of MurA and MurZPages 1730-1734Colin J. Dunsmore, Keith Miller, Katy L. Blake, Simon G. Patching, Peter J.F. Henderson, James A. Garnett, William J. Stubbings, Simon E.V. Phillips, Deborah J. Palestrant, Joseph De Los Angeles, Jennifer A. Leeds, Ian Chopra and Colin W.G. Fishwick
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40.
Separate synthesis and evaluation of glucitol bis-phosphate and mannitol bis-phosphate, as competitive inhibitors of fructose bis-phosphate aldolasesPages 1735-1737Charles-Gabin Mabiala-Bassiloua, Magdalena Zwolinska, Helene Therisod, Jurgen Sygusch and Michel Therisod
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41.
Instructions to contributorsPage I
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