Volume 16; Issue 14

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Bioorganic & Medicinal Chemistry Letters
Volume 16; Issue 14

Bioorganic & Medicinal Chemistry Letters

Volume 16; Issue 14

1

DNA sequence recognition by Hoechst 33258 conjugates of hairpin pyrrole/imidazole polyamides

Bryan J. Correa, Daniele Canzio, Alexandra L. Kahane, Putta Mallikarjuna Reddy, Thomas C. Bruice

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 707 KB

english, 2006

2

QSAR analysis of some 5-amino-2-mercapto-1,3,4-thiadiazole based inhibitors of matrix metalloproteinases and bacterial collagenase

Ashutosh Jamloki, C. Karthikeyan, N.S. Hari Narayana Moorthy, P. Trivedi

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 221 KB

english, 2006

3

Privileged structure based ligands for melanocortin receptors—4,4-Disubstituted piperidine derivatives

Steven L. Kuklish, Ryan T. Backer, Karin Briner, Christopher W. Doecke, Saba Husain, Jeffrey T. Mullaney, Paul L. Ornstein, John M. Zgombick, Thomas P. O’Brien, Matthew J. Fisher

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 117 KB

english, 2006

4

Efforts toward oral bioavailability in factor VIIa inhibitors

Dange Vijaykumar, Roopa Rai, Michael Shaghafi, Tony Ton, Steve Torkelson, Ellen M. Leahy, Jennifer R. Riggs, Huiyong Hu, Paul A. Sprengeler, William D. Shrader, Colin O’Bryan, Ronnell Cabuslay, Ellen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 131 KB

english, 2006

5

3-Substituted gem-cyclohexane sulfone based γ-secretase inhibitors for Alzheimer’s disease: Conformational analysis and biological activity

Richard A. Jelley, Jason Elliott, Karl R. Gibson, Timothy Harrison, Dirk Beher, Earl E. Clarke, Huw D. Lewis, Mark Shearman, Jonathan D.J. Wrigley

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 123 KB

english, 2006

6

Inhibitors of HCV NS5B polymerase: Synthesis and structure–activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring

Todd W. Rockway, Rong Zhang, Dachun Liu, David A. Betebenner, Keith F. McDaniel, John K. Pratt, David Beno, Debra Montgomery, Wen W. Jiang, Sherie Masse, Warren M. Kati, Tim Middleton, Akhteruzzaman M

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 143 KB

english, 2006

7

3D QSAR studies of N-4-arylacryloylpiperazin-1-yl-phenyl-oxazolidinones: A novel class of antibacterial agents

B.B. Lohray, Neha Gandhi, Brijesh Kumar Srivastava, Vidya Bhushan Lohray

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 179 KB

english, 2006

8

Nanomolar inhibition of the enterobactin biosynthesis enzyme, EntE: Synthesis, substituent effects, and additivity

Brian P. Callahan, Joseph V. Lomino, Richard Wolfenden

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 134 KB

english, 2006

9

Novel γ-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates

Yasuko Takahashi, Haruhiko Fuwa, Akane Kaneko, Makoto Sasaki, Satoshi Yokoshima, Hifumi Koizumi, Tohru Takebe, Toshiyuki Kan, Takeshi Iwatsubo, Taisuke Tomita, Hideaki Natsugari, Tohru Fukuyama

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 129 KB

english, 2006

10

Association studies of aggregated aqueous lutein diphosphate with human serum albumin and α1-acid glycoprotein in vitro: Evidence from circular dichroism and electronic absorption spectroscopy

Ferenc Zsila, Geoff Nadolski, Samuel F. Lockwood

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 184 KB

english, 2006

11

Neurotrophic peptide aldehydes: Solid phase synthesis of fellutamide B and a simplified analog

John S. Schneekloth Jr., John L. Sanders, John Hines, Craig M. Crews

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 157 KB

english, 2006

12

Bivalent inhibitors of glutathione S-transferase: The effect of spacer length on isozyme selectivity

Dean Y. Maeda, Sumit S. Mahajan, William M. Atkins, John A. Zebala

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 137 KB

english, 2006

13

Putative therapeutic agents for the learning and memory deficits of people with Down syndrome

Nam Doo Kim, Jeonghyeok Yoon, Jung Ho Kim, Jung Tae Lee, Yong Sog Chon, Mi-Kyung Hwang, Ilho Ha, Woo-Joo Song

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 269 KB

english, 2006

14

Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase

Sheela A. Thomas, Tongmei Li, Keith W. Woods, Xiaohong Song, Garrick Packard, John P. Fischer, Robert B. Diebold, Xuesong Liu, Yan Shi, Vered Klinghofer, Eric F. Johnson, Jennifer J. Bouska, Amanda Ol

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 120 KB

english, 2006

15

Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9

Tadashi Shimamura, Jun Shibata, Hideki Kurihara, Takashi Mita, Sachie Otsuki, Takeshi Sagara, Hiroshi Hirai, Yoshikazu Iwasawa

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 108 KB

english, 2006

16

Novel class of cyclophosphamide prodrug: Cyclophosphamide spiropiperaziniums (CPSP)

Qi Sun, Run-Tao Li, Wei Guo, Jing-Rong Cui, Tie-Ming Cheng, Ze-Mei Ge

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 118 KB

english, 2006

17

Inactivation of GABA transaminase by 4-acryloylphenol

Yun-Hai Tao, Hui-Bi Xu, Xiang-Liang Yang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 131 KB

english, 2006

18

Radical scavenging activities of α-alanine C60 adduct

Tao Sun, Zhude Xu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 111 KB

english, 2006

19

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors

Nigel S. Watson, David Brown, Matthew Campbell, Chuen Chan, Laiq Chaudry, Máire A. Convery, Rebecca Fenwick, J. Nicole Hamblin, Claudine Haslam, Henry A. Kelly, N. Paul King, Cynthia L. Kurtis, Andrew

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 193 KB

english, 2006

20

Markedly enhancing lipase-catalyzed synthesis of nucleoside drugs’ ester by using a mixture system containing organic solvents and ionic liquid

Bo Kai Liu, Na Wang, Zhi Chun Chen, Qi Wu, Xian Fu Lin

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 101 KB

english, 2006

21

Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease

Hiromi Naka, Kenta Teruya, Jeong Kyu Bang, Saburo Aimoto, Tadashi Tatsumi, Hiroyuki Konno, Kazuto Nosaka, Kenichi Akaji

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 129 KB

english, 2006

22

Synthesis of a potential photoactivatable anandamide analog

Laurence Balas, Maria Grazia Cascio, Vincenzo Di Marzo, Thierry Durand

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 119 KB

english, 2006

23

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors

Jagabandhu Das, Joseph A. Furch, Chunjian Liu, Robert V. Moquin, James Lin, Steven H. Spergel, Kim W. McIntyre, David J. Shuster, Kathleen D. O’Day, Becky Penhallow, Chen-Yi Hung, Arthur M. Doweyko, A

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 152 KB

english, 2006

24

Synthesis and structure–activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists

Wen-Lian Wu, Duane A. Burnett, Richard Spring, Li Qiang, Thavalakulamgara K. Sasikumar, Martin S. Domalski, William J. Greenlee, Kim O’Neill, Brian E. Hawes

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 146 KB

english, 2006

25

Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4

Yanfeng Gao, Xin Liu, Weixia Liu, Yuanming Qi, Xuefeng Liu, Yifeng Zhou, Rui Wang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 121 KB

english, 2006

26

Shaken not stirred: A facile synthesis of 1,4-bis(furo[2,3-d]-pyrimidine-2,4(1H,3H)-dione-5-yl)benzenes by one-pot reaction of isocyanides, N,N′-dimethylbarbituric acid, and terephthaldialdehyde

Mohammad Bagher Teimouri, Reihaneh Bazhrang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 153 KB

english, 2006

27

Synthesis, structure analysis, and antitumor activity of 3,6-disubstituted-1,4-dihydro-1,2,4,5-tetrazine derivatives

Guo-Wu Rao, Wei-Xiao Hu

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 134 KB

english, 2006

28

Synthesis and in vitro anti-tumor activity of N-{1-[(3-thioxo-5,6-dihydroimidazo[2,1-c][1,2,4]thiadiazol-7-ylthio)thiocarbonyl]-2-imidazolidene}arylsulfonamides

Jarosław Sączewski, Zdziaław Brzozowski, Franciszek Sączewski, Patrick J. Bednarski, Manuel Liebeke, Maria Gdaniec

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 134 KB

english, 2006

29

Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents

Roland W. Bürli, Han Xu, Xiaoming Zou, Kristine Muller, Jennifer Golden, Mike Frohn, Matthew Adlam, Matthew H. Plant, Min Wong, Michele McElvain, Kelly Regal, Vellarkad N. Viswanadhan, Philip Tagari,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 161 KB

english, 2006

30

Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621

Shenlin Huang, Peter J. Connolly, Ronghui Lin, Stuart Emanuel, Steve A. Middleton

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 147 KB

english, 2006

31

Development of N-4,6-pyrimidine-N-alkyl-N′-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase

Jennifer A. Maier, Todd A. Brugel, Mark Sabat, Adam Golebiowski, Matthew J. Laufersweiler, John C. VanRens, Corey R. Hopkins, Biswanath De, Lily C. Hsieh, Kimberly K. Brown, Vijayasurian Easwaran, Mic

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 138 KB

english, 2006

32

Structure–activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists

Adrian Hall, Stephen Atkinson, Susan H. Brown, Iain P. Chessell, Anita Chowdhury, Nicholas M. Clayton, Tanya Coleman, Gerard M.P. Giblin, Robert J. Gleave, Beverley Hammond, Mark P. Healy, Matthew R.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 148 KB

english, 2006

33

New pyrrolopyrimidin-6-yl benzenesulfonamides: Potent A2B adenosine receptor antagonists

Cristina Esteve, Arsenio Nueda, José Luis Díaz, Jorge Beleta, Alvaro Cárdenas, Estrella Lozoya, Maria Isabel Cadavid, Maria Isabel Loza, Hamish Ryder, Bernat Vidal

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 111 KB

english, 2006

34

BACE-1 inhibition by a series of ψ[CH2NH] reduced amide isosteres

Craig A. Coburn, Shawn J. Stachel, Kristen G. Jones, Thomas G. Steele, Diane M. Rush, Jillian DiMuzio, Beth L. Pietrak, Ming-Tain Lai, Qian Huang, Janet Lineberger, Lixia Jin, Sanjeev Munshi, M. Katha

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 149 KB

english, 2006

35

Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes

Lin Yan, Pei Huo, George Doherty, Lesile Toth, Jeffrey J. Hale, Sander G. Mills, Richard Hajdu, Carol A. Keohane, Mark J. Rosenbach, James A. Milligan, Gan-Ju Shei, Gary Chrebet, James Bergstrom, Debo

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 132 KB

english, 2006

36

Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors

Uma Siripurapu, Renata Kolanos, Małgorzata Dukat, Bryan L. Roth, Richard A. Glennon

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 122 KB

english, 2006

37

Editorial board

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 263 KB

english, 2006

38

Graphical contents list

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 258 KB

english, 2006

39

Instructions to contributors

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 30 KB

english, 2006

40

Synthesis and antibacterial evaluation of ureides of Baylis–Hillman derivatives

Somnath Nag, Richa Pathak, Manish Kumar, P.K. Shukla, Sanjay Batra

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 143 KB

english, 2006

41

Facile synthesis and application of uniformly 13C, 15N-labeled phosphotyrosine for ligand binding studies

Adriaan W. Tuin, Gregg Siegal, Gijsbert A. van der Marel, Herman S. Overkleeft, Dmitri V. Filippov

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 171 KB

english, 2006

42

Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase

Orla K. Mc Carthy, Alessandro Schipani, Alex Musso Buendía, Luis M. Ruiz-Perez, Marcel Kaiser, Reto Brun, Dolores González Pacanowska, Ian H. Gilbert

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 156 KB

english, 2006

43

Cyclobutane derivatives as potent NK1 selective antagonists

Michelle Laci Wrobleski, Gregory A. Reichard, Sunil Paliwal, Sapna Shah, Hon-Chung Tsui, Ruth A. Duffy, Jean E. Lachowicz, Cynthia A. Morgan, Geoffrey B. Varty, Neng-Yang Shih

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 134 KB

english, 2006

44

Crystal structure, spectroscopic, and biological study of the copper(II) complex with third-generation quinolone antibiotic sparfloxacin

Eleni K. Efthimiadou, Yiannis Sanakis, Catherine P. Raptopoulou, Alexandra Karaliota, Nikos Katsaros, George Psomas

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 174 KB

english, 2006

45

3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors

Christopher M. McBride, Paul A. Renhowe, Thomas G. Gesner, Johanna M. Jansen, Julie Lin, Sylvia Ma, Yasheen Zhou, Cynthia M. Shafer

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 148 KB

english, 2006

46

Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa

John M. Fevig, Joseph Cacciola, Joseph Buriak Jr., Karen A. Rossi, Robert M. Knabb, Joseph M. Luettgen, Pancras C. Wong, Stephen A. Bai, Ruth R. Wexler, Patrick Y.S. Lam

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 166 KB

english, 2006

47

Discovery of 3,5-bis(trifluoromethyl)benzyl l-arylglycinamide based potent CCR2 antagonists

Lihu Yang, Changyou Zhou, Liangqin Guo, Gregori Morriello, Gabor Butora, Alexander Pasternak, William H. Parsons, Sander G. Mills, Malcolm MacCoss, Pasquale P. Vicario, Hans Zweerink, Julia M. Ayala,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 150 KB

english, 2006

48

Design of cyclic peptides with agonist activity at melanocortin receptor-4

Takenao Odagami, Yuko Tsuda, Yuji Kogami, Hiroyuki Kouji, Yoshio Okada

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 163 KB

english, 2006

49

Array synthesis of progesterone receptor antagonists: 3-Aryl-1,2-diazepines

Robert W. Wiethe, Eugene L. Stewart, David H. Drewry, David W. Gray, Abdul Mehbob, William J. Hoekstra

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 105 KB

english, 2006

50

Corrigendum to “Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors” [Bioorg. Med. Chem. Lett. 16 (2006) 1643–1646]

Leon Smith II, Evgueni L. Piatnitski, Alexander S. Kiselyov, Xiaohu Ouyang, Xiaoling Chen, Sabina Burdzovic-Wizemann, Yongjiang Xu, Weitao Pan, Xin Chen, Ying Wang, Robin L. Rosler, Sheetal N. Patel,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 59 KB

english, 2006

51

Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists

Wen-Lian Wu, Duane A. Burnett, Mary Ann Caplen, Martin S. Domalski, Chad Bennett, William J. Greenlee, Brian E. Hawes, Kim O’Neill, Blair Weig, Daniel Weston, Brian Spar, Timothy Kowalski

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 131 KB

english, 2006

52

Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor

Petr Vachal, Leslie M. Toth, Jeffrey J. Hale, Lin Yan, Sander G. Mills, Gary L. Chrebet, Carol A. Koehane, Richard Hajdu, James A. Milligan, Mark J. Rosenbach, Suzanne Mandala

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 163 KB

english, 2006

53

Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor

Joe A. Tran, Joseph Pontillo, Beth A. Fleck, Dragan Marinkovic, Melissa Arellano, Fabio C. Tucci, Marion Lanier, John Saunders, Wanlong Jiang, Caroline W. Chen, Alan C. Foster, Chen Chen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 126 KB

english, 2006

54

Nε-Thioacetyl-lysine: A multi-facet functional probe for enzymatic protein lysine Nε-deacetylation

David G. Fatkins, Andrew D. Monnot, Weiping Zheng

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 197 KB

english, 2006

55

Corrigendum to “Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility”: [Bioorg. Med. Chem. Lett. 16 (2006) 443–446]

Jianyong Chen, Ke Ding, Beth Levant, Shaomeng Wang

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

File:

PDF, 48 KB

2006

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