Pyrazole CCK1 receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free–Wilson additivity (English)
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- New search for: Shankley, Nigel
- New search for: Breitenbucher, J. Guy
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In:
Bioorganic and Medicinal Chemistry Letters
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16
, 1
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77-80
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2005
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ISSN:
- Article (Journal) / Electronic Resource
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Title:Pyrazole CCK1 receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free–Wilson additivity
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Contributors:Sehon, Clark ( author ) / McClure, Kelly ( author ) / Hack, Michael ( author ) / Morton, Magda ( author ) / Gomez, Laurent ( author ) / Li, Lina ( author ) / Barrett, Terrance D. ( author ) / Shankley, Nigel ( author ) / Breitenbucher, J. Guy ( author )
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Published in:Bioorganic and Medicinal Chemistry Letters ; 16, 1 ; 77-80
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Publisher:
- New search for: Elsevier Ltd
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Publication date:2005-09-13
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Size:4 pages
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ISSN:
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DOI:
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Type of media:Article (Journal)
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Type of material:Electronic Resource
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Language:English
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Keywords:
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Source:
Table of contents – Volume 16, Issue 1
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.
- 1
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Graphical contents list| 2005
- 15
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Targeting the DNA minor groove with fused ring dicationic compounds: Comparison of in silico screening and a high-resolution crystal structureCampbell, Nancy H. / Evans, David A. / Lee, Michael P.H. / Parkinson, Gary N. / Neidle, Stephen et al. | 2005
- 20
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N-Hydroxyurea as zinc binding group in matrix metalloproteinase inhibition: Mode of binding in a complex with MMP-8Campestre, Cristina / Agamennone, Mariangela / Tortorella, Paolo / Preziuso, Serena / Biasone, Alessandro / Gavuzzo, Enrico / Pochetti, Giorgio / Mazza, Fernando / Hiller, Oliver / Tschesche, Harald et al. | 2005
- 25
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Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2)Ulmschneider, Sarah / Negri, Matthias / Voets, Marieke / Hartmann, Rolf W. et al. | 2005
- 31
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Design, synthesis and in vitro antimalarial activity of an acylhydrazone libraryMelnyk, Patricia / Leroux, Virginie / Sergheraert, Christian / Grellier, Philippe et al. | 2005
- 36
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Peptide inhibitors of dengue virus NS3 protease. Part 1: WarheadYin, Zheng / Patel, Sejal J. / Wang, Wei-Ling / Wang, Gang / Chan, Wai-Ling / Rao, K.R. Ranga / Alam, Jenefer / Jeyaraj, Duraiswamy A. / Ngew, Xinyi / Patel, Viral et al. | 2005
- 40
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Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitorsYin, Zheng / Patel, Sejal J. / Wang, Wei-Ling / Chan, Wai-Ling / Ranga Rao, K.R. / Wang, Gang / Ngew, Xinyi / Patel, Viral / Beer, David / Knox, John E. et al. | 2005
- 44
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Synthesis and biological activity of novel 4-phenyl-1,8-naphthyridin-2(1H)-on-3-yl ureas: Potent acyl-CoA:cholesterol acyltransferase inhibitor with improved aqueous solubilityBan, Hitoshi / Muraoka, Masami / Ioriya, Katsuhisa / Ohashi, Naohito et al. | 2005
- 49
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Synthesis of the PPARβ/δ-selective agonist GW501516 and C4-thiazole-substituted analogsPereira, Raquel / Gaudon, Claudine / Iglesias, Beatriz / Germain, Pierre / Gronemeyer, Hinrich / de Lera, Angel R. et al. | 2005
- 49
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Synthesis of the PPAR#946-#948-selective agonist GW501516 and C4-thiazole-substituted analogsPereira, Raquel et al. | 2006
- 55
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Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivativeKinoshita, Takayoshi / Warizaya, Masaichi / Ohori, Makoto / Sato, Kentaro / Neya, Masahiro / Fujii, Takashi et al. | 2005
- 59
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3-Substituted indolizine-1-carbonitrile derivatives as phosphatase inhibitorsWeide, Timo / Arve, Lars / Prinz, Heino / Waldmann, Herbert / Kessler, Horst et al. | 2005
- 64
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p38 MAP kinase inhibitors: Metabolically stabilized piperidine-substituted quinolinones and naphthyridinonesBao, Jianming / Hunt, Julianne A. / Miao, Shouwu / Rupprecht, Kathleen M. / Stelmach, John E. / Liu, Luping / Ruzek, Rowena D. / Sinclair, Peter J. / Pivnichny, James V. / Hop, Cornelis E.C.A. et al. | 2005
- 69
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Hexylitaconic acid: A new inhibitor of p53–HDM2 interaction isolated from a marine-derived fungus, Arthrinium sp.Tsukamoto, Sachiko / Yoshida, Takushi / Hosono, Hidetaka / Ohta, Tomihisa / Yokosawa, Hideyoshi et al. | 2005
- 69
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Hexylitaconic acid: A new inhibitor of p53#8211HDM2 interaction isolated from a marine-derived fungus, Arthrinium sp.Tsukamoto, Sachiko et al. | 2006
- 72
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Pyrazole CCK1 receptor antagonists. Part 1: Solution-phase library synthesis and determination of Free#8211Wilson additivityMcclure, Kelly et al. | 2006
- 72
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Pyrazole CCK1 receptor antagonists. Part 1: Solution-phase library synthesis and determination of Free–Wilson additivityMcClure, Kelly / Hack, Michael / Huang, Liming / Sehon, Clark / Morton, Magda / Li, Lina / Barrett, Terrance D. / Shankley, Nigel / Breitenbucher, J. Guy et al. | 2005
- 77
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Pyrazole CCK1 receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free–Wilson additivitySehon, Clark / McClure, Kelly / Hack, Michael / Morton, Magda / Gomez, Laurent / Li, Lina / Barrett, Terrance D. / Shankley, Nigel / Breitenbucher, J. Guy et al. | 2005
- 77
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Pyrazole CCK1 receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free#8211Wilson additivitySehon, Clark et al. | 2006
- 81
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Safrole oxide induces apoptosis by activating caspase-3, -8, and -9 in A549 human lung cancer cellsDu, AiYing / Zhao, BaoXiang / Yin, DeLing / Zhang, ShangLi / Miao, JunYing et al. | 2005
- 84
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NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studiesEttmayer, Peter / Baumruker, Thomas / Guerini, Danilo / Mechtcheriakova, Diana / Nussbaumer, Peter / Streiff, Markus B. / Billich, Andreas et al. | 2005
- 88
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The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenaseHeikkilä, Timo / Thirumalairajan, Srinath / Davies, Matthew / Parsons, Mark R. / McConkey, A. Glenn / Fishwick, Colin W.G. / Johnson, A. Peter et al. | 2005
- 93
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Analogues of N-terminal truncated synthetic peptide fragments derived from RANTES inhibit HIV-1 infectivityRamnarine, Emabelle J. / DeVico, Anthony L. / Vigil-Cruz, Sandra C. et al. | 2005
- 96
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Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitorsAkritopoulou-Zanze, Irini / Darczak, Daria / Sarris, Kathy / Phelan, Kathleen M. / Huth, Jeffrey R. / Song, Danying / Johnson, Eric F. / Jia, Yong / Djuric, Stevan W. et al. | 2005
- 100
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Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymeraseLaPorte, M.G. / Lessen, T.A. / Leister, L. / Cebzanov, D. / Amparo, E. / Faust, C. / Ortlip, D. / Bailey, T.R. / Nitz, T.J. / Chunduru, S.K. et al. | 2005
- 104
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The design, synthesis, and evaluation of two universal doxorubicin-linkers: Preparation of conjugates that retain topoisomerase II activitySun, Chengzao / Aspland, Simon E. / Ballatore, Carlo / Castillo, Rosario / Smith, Amos B. III / Castellino, Angelo J. et al. | 2005
- 108
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Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKKWaelchli, Rudolf / Bollbuck, Birgit / Bruns, Christian / Buhl, Thomas / Eder, Jörg / Feifel, Roland / Hersperger, Rene / Janser, Philipp / Revesz, Laszlo / Zerwes, Hans-Günter et al. | 2005
- 113
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Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agentsCoppola, Gary M. / Damon, Robert E. / Eskesen, J. Bruce / France, Dennis S. / Paterniti, James R. Jr. et al. | 2005
- 118
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Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejectionBurchat, Andrew / Borhani, David W. / Calderwood, David J. / Hirst, Gavin C. / Li, Biqin / Stachlewitz, Robert F. et al. | 2005
- 123
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Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitorsQiao, Lei / Baumann, Christian A. / Crysler, Carl S. / Ninan, Nisha S. / Abad, Marta C. / Spurlino, John C. / DesJarlais, Renee L. / Kervinen, Jukka / Neeper, Mike P. / Bayoumy, Shariff S. et al. | 2005
- 129
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Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinasesHan, Sun-Young / Park, Seok-Soon / Lee, Woo Ghil / Min, Yong Ki / Kim, Bum Tae et al. | 2005
- 134
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Design and synthesis of downsized metastin (45–54) analogs with maintenance of high GPR54 agonistic activityNiida, Ayumu / Wang, Zixuan / Tomita, Kenji / Oishi, Shinya / Tamamura, Hirokazu / Otaka, Akira / Navenot, Jean-Marc / Broach, James R. / Peiper, Stephen C. / Fujii, Nobutaka et al. | 2005
- 134
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Design and synthesis of downsized metastin (45#821154) analogs with maintenance of high GPR54 agonistic activityNiida, Ayumu et al. | 2006
- 138
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New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studiesUrbani, Paolo / Cavallo, Paolo / Cascio, Maria Grazia / Buonerba, Mariafrancesca / De Martino, Giovanni / Di Marzo, Vincenzo / Saturnino, Carmela et al. | 2005
- 142
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The structure–activity relationships of mansonone F, a potent anti-MRSA sesquiterpenoid quinone: SAR studies on the C6 and C9 analogsSuh, Young-Ger / Kim, Sun Nam / Shin, Dong-Yun / Hyun, Soon-Sil / Lee, Do-Sang / Min, Kyung-Hoon / Han, Sae Mi / Li, Funan / Choi, Eung-Chil / Choi, Seong-Hak et al. | 2005
- 142
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The structure#8211activity relationships of mansonone F, a potent anti-MRSA sesquiterpenoid quinone: SAR studies on the C6 and C9 analogsSuh, Young-Ger et al. | 2006
- 146
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4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective δ-opioid agonistsTrabanco, Andrés A. / Pullan, Shirley / Alonso, José M. / Alvarez, Rosa M. / Andrés, José I. / Boeckx, Inge / Fernández, Javier / Gómez, Antonio / Iturrino, Laura / Janssens, Frans E. et al. | 2005
- 146
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4-Phenyl-4-(1H-imidazol-2-yl)-piperidine derivatives, a novel class of selective #948-opioid agonistsTrabanco, Andrés A. et al. | 2006
- 150
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3-Arylpiperazinylethyl-1H-pyrrolo(2,3-d)pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective #9451-adrenoceptor ligandsPittalà, Valeria et al. | 2006
- 150
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3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective α1-adrenoceptor ligandsPittalà, Valeria / Romeo, Giuseppe / Salerno, Loredana / Siracusa, Maria Angela / Modica, Maria / Materia, Luisa / Mereghetti, Ilario / Cagnotto, Alfredo / Mennini, Tiziana / Marucci, Gabriella et al. | 2005
- 154
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Photoreactive threading agent that specifically binds to abasic sites in DNAMartelli, Alain / Jourdan, Muriel / Constant, Jean-François / Demeunynck, Martine / Dumy, Pascal et al. | 2005
- 158
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Affinity identification of δ-opioid receptors using latex nanoparticlesHasegawa, Makoto / Ohno, Hiroshi / Tanaka, Hiroshi / Hatakeyama, Mamoru / Kawaguchi, Haruma / Takahashi, Takashi / Handa, Hiroshi et al. | 2005
- 158
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Affinity identification of #948-opioid receptors using latex nanoparticlesHasegawa, Makoto et al. | 2006
- 162
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A novel class of potent influenza virus inhibitors: Polysubstituted acylthiourea and its fused heterocycle derivativesSun, Chuanwen / Huang, Hai / Feng, Meiqing / Shi, Xunlong / Zhang, Xiaodong / Zhou, Pei et al. | 2005
- 167
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New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonistsZappalà, Maria / Pellicanò, Alessia / Micale, Nicola / Menniti, Frank S. / Ferreri, Guido / De Sarro, Giovambattista / Grasso, Silvana / De Micheli, Carlo et al. | 2005
- 171
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Synthesis and biological evaluation of novel heterocyclic quinones as inhibitors of the dual specificity protein phosphatase CDC25CLavergne, Olivier / Fernandes, Anne-Cécile / Bréhu, Laetitia / Sidhu, Alban / Brézak, Marie-Christine / Prévost, Grégoire / Ducommun, Bernard / Contour-Galcera, Marie-Odile et al. | 2005
- 176
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Pulvinones as bacterial cell wall biosynthesis inhibitorsAntane, Schuyler / Caufield, Craig E. / Hu, William / Keeney, David / Labthavikul, Pornpen / Morris, Koi / Naughton, Shaughnessy M. / Petersen, Peter J. / Rasmussen, Beth A. / Singh, Guy et al. | 2005
- 181
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C8c#8211C15 monoseco-analogues of the phenanthroquinolizidine alkaloids julandine and cryptopleurine exhibiting potent anti-angiogenic propertiesBanwell, Martin G. et al. | 2006
- 181
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C8c–C15 monoseco-analogues of the phenanthroquinolizidine alkaloids julandine and cryptopleurine exhibiting potent anti-angiogenic propertiesBanwell, Martin G. / Bezos, Anna / Burns, Christopher / Kruszelnicki, Irma / Parish, Christopher R. / Su, Stephen / Sydnes, Magne O. et al. | 2005
- 186
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Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5]Bennett, Frank / Saksena, Anil K. / Lovey, Raymond G. / Liu, Yi-Tsung / Patel, Naginbhai M. / Pinto, Patrick / Pike, Russel / Jao, Edwin / Girijavallabhan, Viyyoor M. / Ganguly, Ashit K. et al. | 2005
- 191
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Macrocyclic peptidomimetic inhibitors of #946-secretase (BACE): First X-ray structure of a macrocyclic peptidomimetic-BACE complexRojo, Isabel et al. | 2006
- 191
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Macrocyclic peptidomimetic inhibitors of β-secretase (BACE): First X-ray structure of a macrocyclic peptidomimetic-BACE complexRojo, Isabel / Martín, José Alfredo / Broughton, Howard / Timm, David / Erickson, Jon / Yang, Hsiu-Chiung / McCarthy, James R. et al. | 2005
- 196
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Synthesis and preliminary biological evaluation of (2S,1′R,2′S)- and (2S,1′S,2′R)-2-(2′-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analoguesAmori, Laura / Serpi, Michaela / Marinozzi, Maura / Costantino, Gabriele / Diaz, Monica Gavilan / Hermit, Mette Brunsgaard / Thomsen, Christian / Pellicciari, Roberto et al. | 2005
- 196
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Synthesis and preliminary biological evaluation of (2S,1#8242R,2#8242S)- and (2S,1#8242S,2#8242R)-2-(2#8242-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analoguesAmori, Laura et al. | 2006
- 200
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Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonistsCole, Andrew G. / Stroke, Ilana L. / Brescia, Marc-Raleigh / Simhadri, Srilatha / Zhang, Joan J. / Hussain, Zahid / Snider, Michael / Haskell, Christopher / Ribeiro, Sofia / Appell, Kenneth C. et al. | 2005
- 204
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Optimization of CCR4 antagonists: Side-chain explorationPurandare, Ashok V. / Wan, Honghe / Gao, Aiming / Somerville, John / Burke, Christine / Vaccaro, Wayne / Yang, XiaoXia / McIntyre, Kim W. / Poss, Michael A. et al. | 2005
- 208
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In vitro photo-release of a TRPV1 agonistCarr, James L. / Wease, Kerrie N. / Van Ryssen, Michael P. / Paterson, Suzanne / Agate, Ben / Gallagher, Katherine A. / Brown, C. Tom A. / Scott, Roderick H. / Conway, Stuart J. et al. | 2005
- 213
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Modular polyketide synthases: Investigating intermodular communication using 6 deoxyerythronolide B synthase module 2Moffet, David A. / Khosla, Chaitan / Cane, David E. et al. | 2005
- 217
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Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropanesTamagnan, Gilles / Alagille, David / Fu, Xing / Kula, Nora S. / Baldessarini, Ross J. / Innis, Robert B. / Baldwin, Ronald M. et al. | 2005
- 217
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Synthesis and monoamine transporter affinity of new 2#946-carbomethoxy-3#946-(aryl or heteroaryl)phenyltropanesTamagnan, Gilles et al. | 2006
- 221
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Synthesis and biological evaluation of novel C (7) modified chrysin analogues as antibacterial agentsSuresh Babu, K. / Hari Babu, T. / Srinivas, P.V. / Hara Kishore, K. / Murthy, U.S.N. / Rao, J. Madhusudana et al. | 2005
- 225
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Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I)Zheng, Jianbin / Wen, Ren / Luo, Xiaomin / Lin, Guoqiang / Zhang, Jiange / Xu, Linfeng / Guo, Lihe / Jiang, Hualiang et al. | 2005
- 228
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The crystal structures of 3-TAPAP in complexes with the urokinase-type plasminogen activator and picrateŻesławska, Ewa / Jacob, Uwe / Stürzebecher, Jörg / Oleksyn, Barbara J. et al. | 2005
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Editorial board| 2005
- I
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Summary of Instructions to Authors| 2005