Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: In vitro profiling and in vivo evaluation (English)
- New search for: Semple, Graeme
- New search for: Semple, Graeme
- New search for: Tran, Thuy-Anh
- New search for: Kramer, Bryan
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- New search for: Casper, Martin D.
- New search for: Zou, Ning
- New search for: Hauser, Erin K.
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In:
Bioorganic & medicinal chemistry letters
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19
, 21
; 6166-6171
;
2009
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ISSN:
- Article (Journal) / Print
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Title:Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: In vitro profiling and in vivo evaluation
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Contributors:Semple, Graeme ( author ) / Tran, Thuy-Anh / Kramer, Bryan / Hsu, Debbie / Han, Sangdon / Choi, Juyi / Vallar, Pureza / Casper, Martin D. / Zou, Ning / Hauser, Erin K.
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Published in:Bioorganic & medicinal chemistry letters ; 19, 21 ; 6166-6171
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Publisher:
- New search for: Elsevier
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Place of publication:Amsterdam [u.a.]
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Publication date:2009
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ISSN:
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ZDBID:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
- New search for: 35.70 / 44.33 / 44.42
- Further information on Basic classification
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Source:
Table of contents – Volume 19, Issue 21
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 5975
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Graphical contents list| 2009
- 5990
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Insights into the inhibition of xanthine oxidase by curcuminShen, Liang / Ji, Hong-Fang et al. | 2009
- 5994
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N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: The development of diaryl amino piperidines as potent d opioid receptor agonists with in vivo anti-nociceptive activity in rodent modelsJones, P. / Griffin, A. M. / Gawell, L. / Lavoie, R. / Delorme, D. / Roberts, E. / Brown, W. / Walpole, C. / Xiao, W. / Boulet, J. et al. | 2009
- 5994
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N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: The development of diaryl amino piperidines as potent δ opioid receptor agonists with in vivo anti-nociceptive activity in rodent modelsJones, Paul / Griffin, Andrew M. / Gawell, Lars / Lavoie, Rico / Delorme, Daniel / Roberts, Edward / Brown, William / Walpole, Christopher / Xiao, Wenhau / Boulet, Jamie et al. | 2009
- 5999
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Delta agonist hydroxy bioisosteres: The discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stabilityGriffin, Andrew M. / Brown, William / Walpole, Christopher / Coupal, Martin / Adam, Lynda / Gosselin, Mylene / Salois, Dominic / Morin, Pierre-Emmanuel / Roumi, Marie et al. | 2009
- 6004
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Synthesis and biological evaluation of berberine analogues as novel up-regulators for both low-density-lipoprotein receptor and insulin receptorWang, Yan-Xiang / Wang, Yu-Ping / Zhang, Hao / Kong, Wei-Jia / Li, Ying-Hong / Liu, Fei / Gao, Rong-Mei / Liu, Ting / Jiang, Jian-Dong / Song, Dan-Qing et al. | 2009
- 6009
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Glucose-containing flavones—their synthesis and antioxidant and neuroprotective activitiesKim, Seung Hwan / Naveen Kumar, Ch. / Kim, Hyoung Ja / Kim, Dong Han / Cho, Jungsook / Jin, Changbae / Lee, Yong Sup et al. | 2009
- 6014
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Carbonic anhydrase II-induced selection of inhibitors from a dynamic combinatorial library of Schiff’s basesNasr, Gihane / Petit, Eddy / Supuran, Claudiu T. / Winum, Jean-Yves / Barboiu, Mihail et al. | 2009
- 6018
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Tetrahydroquinoline sulfonamides as vasopressin 1b receptor anatgonistsScott, Jack D. / Miller, Michael W. / Li, Sarah W. / Lin, Sue-Ing / Vaccaro, Henry A. / Hong, Liwu / Mullins, Deborra E. / Guzzi, Mario / Weinstein, Jay / Hodgson, Robert A. et al. | 2009
- 6023
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Evaluation of triazolamers as active site inhibitors of HIV-1 proteaseJochim, Andrea L. / Miller, Stephen E. / Angelo, Nicholas G. / Arora, Paramjit S. et al. | 2009
- 6027
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Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat modelHo, Koc-Kan / Beasley, James R. / Belanger, Laura / Black, Darcey / Chan, Jui-Hsiang / Dunn, David / Hu, Bing / Klon, Anthony / Kultgen, Steven G. / Ohlmeyer, Michael et al. | 2009
- 6032
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Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liabilityJosien, Hubert / Bara, Thomas / Rajagopalan, Murali / Clader, John W. / Greenlee, William J. / Favreau, Leonard / Hyde, Lynn A. / Nomeir, Amin A. / Parker, Eric M. / Song, Lixin et al. | 2009
- 6032
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Novel orally active morpholine N-arylsulfonamides g-secretase inhibitors with low CYP 3A4 liabilityJosien, H. / Bara, T. / Rajagopalan, M. / Clader, J. W. / Greenlee, W. J. / Favreau, L. / Hyde, L. A. / Nomeir, A. A. / Parker, E. M. / Song, L. et al. | 2009
- 6038
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Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformationShi, Jin / Stover, James S. / Whitby, Landon R. / Vogt, Peter K. / Boger, Dale L. et al. | 2009
- 6042
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Structure–activity relationship (SAR) studies of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione: Development of potential substrate-specific ERK1/2 inhibitorsLi, Qianbin / Al-Ayoubi, Adnan / Guo, Tailiang / Zheng, Hui / Sarkar, Aurijit / Nguyen, Tri / Eblen, Scott T. / Grant, Steven / Kellogg, Glen E. / Zhang, Shijun et al. | 2009
- 6047
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5,5prime- and 6,6prime-Dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymeraseEllis, D. A. / Blazel, J. K. / Tran, C. V. / Ruebsam, F. / Murphy, D. E. / Li, L. S. / Zhao, J. / Zhou, Y. / McGuire, H. M. / Xiang, A. X. et al. | 2009
- 6047
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5,5′- and 6,6′-Dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymeraseEllis, David A. / Blazel, Julie K. / Tran, Chinh V. / Ruebsam, Frank / Murphy, Douglas E. / Li, Lian-Sheng / Zhao, Jingjing / Zhou, Yuefen / McGuire, Helen M. / Xiang, Alan X. et al. | 2009
- 6053
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Synthesis and structure–activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonistsLee, Ju-Yeon / Yu, Juan / Cho, Won Je / Ko, Hyojin / Kim, Yong-Chul et al. | 2009
- 6059
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Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motifCarro, Laura / Raviña, Enrique / Domínguez, Eduardo / Brea, José / Loza, María I. / Masaguer, Christian F. et al. | 2009
- 6063
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Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitorsKang, Iou-Jiun / Wang, Li-Wen / Hsu, Sheng-Ju / Lee, Chung-Chi / Lee, Yen-Chun / Wu, Yen-Shian / Yueh, Andrew / Wang, Jing-Chyi / Hsu, Tsu-An / Chao, Yu-Sheng et al. | 2009
- 6069
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Facile synthesis of anthracene-appended amino acids as highly selective and sensitive fluorescent Fe3+ ion sensorsLohani, Chuda Raj / Kim, Joung-Min / Lee, Keun-Hyeung et al. | 2009
- 6074
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Synthesis and evaluation of (S,S)-N,N′-bis-[3-(2,2′,6,6′-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activityZhang, Xuelian / Hu, Yanwei / Chen, Shudan / Luo, Rusong / Yue, Jun / Zhang, Ying / Duan, Wenhu / Wang, Honghai et al. | 2009
- 6074
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Synthesis and evaluation of (S,S)-N,Nprime-bis-[3-(2,2prime,6,6prime-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activityZhang, X. / Hu, Y. / Chen, S. / Luo, R. / Yue, J. / Zhang, Y. / Duan, W. / Wang, H. et al. | 2009
- 6078
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Phytochemical investigation of labdane diterpenes from the rhizomes of Hedychium spicatum and their cytotoxic activityPrabhakar Reddy, P. / Ranga Rao, R. / Shashidhar, J. / Sastry, B.S. / Madhusudana Rao, J. / Suresh Babu, K. et al. | 2009
- 6082
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Cellular signal-specific peptide substrate is essential for the gene delivery system responding to cellular signalsKang, Jeong-Hun / Toita, Riki / Tomiyama, Tetsuro / Oishi, Jun / Asai, Daisuke / Mori, Takeshi / Niidome, Takuro / Katayama, Yoshiki et al. | 2009
- 6087
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A dynamic target-based pharmacophoric model mapping the CD4 binding site on HIV-1 gp120 to identify new inhibitors of gp120–CD4 protein–protein interactionsCaporuscio, Fabiana / Tafi, Andrea / González, Emmanuel / Manetti, Fabrizio / Esté, José A. / Botta, Maurizio et al. | 2009
- 6092
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Hydrogen sulfide induces nitric oxide release from nitriteGrossi, Loris et al. | 2009
- 6095
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Isolation of the protein tyrosine phosphatase 1B inhibitory metabolite from the marine-derived fungus Cosmospora sp. SF-5060Seo, Changon / Sohn, Jae Hak / Oh, Hyuncheol / Kim, Bo Yeon / Ahn, Jong Seog et al. | 2009
- 6098
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Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinasesEnkvist, Erki / Kriisa, Marie / Roben, Mart / Kadak, Grete / Raidaru, Gerda / Uri, Asko et al. | 2009
- 6102
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Analogs of a 4-aminothieno[2,3-d]pyrimidine lead (QB13) as modulators of P-glycoprotein substrate specificityHäcker, Hans-Georg / Haye, Antje de la / Sterz, Katja / Schnakenburg, Gregor / Wiese, Michael / Gütschow, Michael et al. | 2009
- 6106
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Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonistsMartin, Rainer E. / Mohr, Peter / Maerki, Hans Peter / Guba, Wolfgang / Kuratli, Christoph / Gavelle, Olivier / Binggeli, Alfred / Bendels, Stefanie / Alvarez-Sánchez, Rubén / Alker, André et al. | 2009
- 6114
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Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives: Their cytoprotection effect from rotenone toxicity and preliminary DMPK propertiesZhou, Yuefen / Liu, Gang / Chen, Jinhua / Murali Mohan Reddy, P.S. / Yoon, Il Sang / Zhang, Menghua / Zhang, Bin / Barber, Jack R. / Ng, Shi Chung et al. | 2009
- 6119
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Discovery of novel sphingosine kinase 1 inhibitorsXiang, Yibin / Asmussen, Gary / Booker, Michael / Hirth, Bradford / Kane, John L. Jr. / Liao, Junkai / Noson, Kevin D. / Yee, Christopher et al. | 2009
- 6122
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Structure–activity relationship study of EphB3 receptor tyrosine kinase inhibitorsQiao, Lixin / Choi, Sungwoon / Case, April / Gainer, Thomas G. / Seyb, Kathleen / Glicksman, Marcie A. / Lo, Donald C. / Stein, Ross L. / Cuny, Gregory D. et al. | 2009
- 6127
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Efficient synthesis of nevirapine analogs to study its metabolic profile by click fishingBernard, Sylvain / Defoy, Daniel / Dory, Yves L. / Klarskov, Klaus et al. | 2009
- 6131
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Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elementsAmeriks, Michael K. / Axe, Frank U. / Bembenek, Scott D. / Edwards, James P. / Gu, Yin / Karlsson, Lars / Randal, Mike / Sun, Siquan / Thurmond, Robin L. / Zhu, Jian et al. | 2009
- 6135
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Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: Optimization of cellular potencyAmeriks, Michael K. / Cai, Hui / Edwards, James P. / Gebauer, Damara / Gleason, Elizabeth / Gu, Yin / Karlsson, Lars / Nguyen, Steven / Sun, Siquan / Thurmond, Robin L. et al. | 2009
- 6140
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Puupehanol, a sesquiterpene-dihydroquinone derivative from the marine sponge Hyrtios sp.Xu, Wen-Hui / Ding, Yuanqing / Jacob, Melissa R. / Agarwal, Ameeta K. / Clark, Alice M. / Ferreira, Daneel / Liang, Zong-Suo / Li, Xing-Cong et al. | 2009
- 6144
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Optimising metabolic stability in lipophilic chemical space: The identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonistMiller, Duncan C. / Klute, Wolfgang / Calabrese, Andrew / Brown, Alan D. et al. | 2009
- 6148
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Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregationParlow, John J. / Burney, Mary W. / Case, Brenda L. / Girard, Thomas J. / Hall, Kerri A. / Hiebsch, Ronald R. / Huff, Rita M. / Lachance, Rhonda M. / Mischke, Deborah A. / Rapp, Stephen R. et al. | 2009
- 6157
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Discovery of 4-functionalized phenyl-O-b-d-glycosides as a new class of mushroom tyrosinase inhibitorsYi, W. / Cao, R. / Wen, H. / Yan, Q. / Zhou, B. / Ma, L. / Song, H. et al. | 2009
- 6157
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Discovery of 4-functionalized phenyl-O-β-d-glycosides as a new class of mushroom tyrosinase inhibitorsYi, Wei / Cao, Rihui / Wen, Huan / Yan, Qin / Zhou, Binhua / Ma, Lin / Song, Huacan et al. | 2009
- 6161
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Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effectsBhattarai, Bharat Raj / Kafle, Bhooshan / Hwang, Ji-Sun / Khadka, Deegendra / Lee, Sun-Myung / Kang, Jae-Seung / Ham, Seung Wook / Han, Inn-Oc / Park, Hwangseo / Cho, Hyeongjin et al. | 2009
- 6166
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Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: In vitro profiling and in vivo evaluationSemple, Graeme / Tran, Thuy-Anh / Kramer, Bryan / Hsu, Debbie / Han, Sangdon / Choi, Juyi / Vallar, Pureza / Casper, Martin D. / Zou, Ning / Hauser, Erin K. et al. | 2009
- 6172
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New inhibitors of the complement system inspired in K76-COOH. A SAR study of filifolinol derivatives through modifications of the C3′ positionLarghi, Enrique L. / Operto, María A. / Torres, Rene / Kaufman, Teodoro S. et al. | 2009
- 6172
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New inhibitors of the complement system inspired in K76-COOH. A SAR study of filifolinol derivatives through modifications of the C3prime positionLarghi, E. L. / Operto, M. A. / Torres, R. / Kaufman, T. S. et al. | 2009
- 6176
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Synthesis and structure-activity relationships of 2-(1,4prime-bipiperidin-1prime-yl)thiazolopyridine as H3 receptor antagonistsRao, A. U. / Palani, A. / Chen, X. / Huang, Y. / Aslanian, R. G. / West, R. E. / Williams, S. M. / Wu, R. L. / Hwa, J. / Sondey, C. et al. | 2009
- 6176
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Synthesis and structure–activity relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridine as H3 receptor antagonistsRao, Ashwin U. / Palani, Anandan / Chen, Xiao / Huang, Ying / Aslanian, Robert G. / West, Robert E. Jr. / Williams, Shirley M. / Wu, Ren-Long / Hwa, Joyce / Sondey, Christopher et al. | 2009
- 6181
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Cellular localization and allele-selective inhibition of mutant huntingtin protein by peptide nucleic acid oligomers containing the fluorescent nucleobase [bis-o-(aminoethoxy)phenyl]pyrrolocytosineHu, Jiaxin / Dodd, David W. / Hudson, Robert H.E. / Corey, David R. et al. | 2009
- 6185
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Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: Discovery, characterization and preliminary SAR of a promising leadThoma, Gebhard / Baenteli, Rolf / Lewis, Ian / Wagner, Trixie / Oberer, Lukas / Blum, Wolfgang / Glickman, Fraser / Streiff, Markus B. / Zerwes, Hans-Guenter et al. | 2009
- 6189
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Functional and biochemical analysis of a key series of ramoplanin analoguesFang, Xiao / Nam, Joonwoo / Shin, Dongwoo / Rew, Yosup / Boger, Dale L. / Walker, Suzanne et al. | 2009
- 6192
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2-Oxoglutarate analogue inhibitors of prolyl hydroxylase domain 2Mecinović, Jasmin / Loenarz, Christoph / Chowdhury, Rasheduzzaman / Schofield, Christopher J. et al. | 2009
- 6196
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Discovery of a potent, metabolically stabilized resorcylic lactone as an anti-inflammatory leadDu, H. / Matsushima, T. / Spyvee, M. / Goto, M. / Shirota, H. / Gusovsky, F. / Chiba, K. / Kotake, M. / Yoneda, N. / Eguchi, Y. et al. | 2009
- 6200
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A naturally occurring brominated furanone covalently modifies and inactivates LuxSZang, Tianzhu / Lee, Bobby W.K. / Cannon, Lisa M. / Ritter, Kathryn A. / Dai, Shujia / Ren, Dacheng / Wood, Thomas K. / Zhou, Zhaohui Sunny et al. | 2009
- 6205
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Bicyclic α,ω-dicarboxylic acid derivatives from a colonial tunicate of the family PolyclinidaeBao, Baoquan / Dang, Hung The / Zhang, Ping / Hong, Jongki / Lee, Chong-O. / Cho, Hee Young / Jung, Jee H. et al. | 2009
- 6205
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Bicyclic a,-dicarboxylic acid derivatives from a colonial tunicate of the family PolyclinidaeBao, B. / Dang, H. T. / Zhang, P. / Hong, J. / Lee, C. O. / Cho, H. Y. / Jung, J. H. et al. | 2009
- 6209
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Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptorsDonohue, Sean R. / Varnäs, Katarina / Jia, Zhisheng / Gulyás, Balázs / Pike, Victor W. / Halldin, Christer et al. | 2009
- 6213
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Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitorsShiozaki, Makoto / Imai, Hiroto / Maeda, Katsuya / Miura, Tomoya / Yasue, Katsutaka / Suma, Akira / Yokota, Masahiro / Ogoshi, Yosuke / Haas, Julia / Fryer, Andrew M. et al. | 2009
- 6218
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Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteasesBryant, Clifford / Kerr, Iain D. / Debnath, Moumita / Ang, Kenny K.H. / Ratnam, Joseline / Ferreira, Rafaela S. / Jaishankar, Priyadarshini / Zhao, DongMei / Arkin, Michelle R. / McKerrow, James H. et al. | 2009
- 6222
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Synthesis of (R,S)-[4-11C]baclofen via Michael addition of nitromethane labeled with short-lived 11CKato, Koichi / Zhang, Ming-Rong / Suzuki, Kazutoshi et al. | 2009
- 6225
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Discovery of 3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051-a xanthine oxidoreductase inhibitor for the treatment of hyperuricemiaSato, Takahiro / Ashizawa, Naoki / Matsumoto, Koji / Iwanaga, Takashi / Nakamura, Hiroshi / Inoue, Tsutomu / Nagata, Osamu et al. | 2009
- 6230
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Inhibitor profiling of the Pseudomonas aeruginosa virulence factor LasB using N-alpha mercaptoamide template-based inhibitorsCathcart, George R. / Gilmore, Brendan F. / Greer, Brett / Harriott, Pat / Walker, Brian et al. | 2009
- 6233
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Inhibition of ErbB2(Her2) expression with small molecule transcription factor mimicsLee, Lori W. / Taylor, Christopher E.C. / Desaulniers, Jean-Paul / Zhang, Manchao / Højfeldt, Jonas W. / Pan, Quintin / Mapp, Anna K. et al. | 2009
- 6237
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Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonistsPasternak, Alexander / Goble, Stephen D. / deJesus, Reynalda K. / Hreniuk, Donna L. / Chung, Christine C. / Tota, Michael R. / Mazur, Paul / Feighner, Scott D. / Howard, Andrew D. / Mills, Sander G. et al. | 2009
- 6241
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Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiolAgoston, Gregory E. / Shah, Jamshed H. / Suwandi, Lita / Hanson, Arthur D. / Zhan, Xiaoguo / LaVallee, Theresa M. / Pribluda, Victor / Treston, Anthony M. et al. | 2009
- 6245
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2-(3-Thienyl)-5,6-dihydroxypyrimidine-4-carboxylic acids as inhibitors of HCV NS5B RdRpPacini, Barbara / Avolio, Salvatore / Ercolani, Caterina / Koch, Uwe / Migliaccio, Giovanni / Narjes, Frank / Pacini, Laura / Tomei, Licia / Harper, Steven et al. | 2009
- IFC
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Editorial board| 2009