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117. Synthesis and SAR studies on novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase enzyme. M. Ding,F.He, X. Zheng, T. W. Hudyma, M. A. Poss, J. F. Kadow, K. L. Rigat, Y. Wang, R. Fridell, D. Qiu, M. Liu, S. Boss, M. Gao, S. B. Roberts, R. G. Gentles 118. Synthesis and biological evaluation of the selective inverse agonist PWZ-029 for alpha 5 Bzr/GABA aergic receptor subtypes: This ligand enhances cognition in rhesus monkeys. S. K. Rallapalli, C. Moran, J. K. Rowlett, J. M. Cook 119. Highly potent inhibitors of HCV NS3 protease. B. Venables, N. Sin, A. Wang, L. Sun, D. Hernandez, A. Sheaffer, M. Lee, D. Barry, J. Friborg, F. Yu, J. Knipe, J. Sandquist, A. C. Good, F. Mcphee, N. A. Meanwell, P. M. Scola 120. Design and synthesis of deuterated boceprevir analogs with enhanced pharmacokinetic properties. A. J. Morgan, C. E. Masse, S. Nguyen, V. Uttamsingh, R. Tung, S. Harbeson 121. Rational design, virtual screening, synthesis and biological activity of donepezil-based new acetylcholinesterase inhibitors. S. Datta, D. Borkin, A. Rudnitskaya, M. Torok, B. Torok 122. Application of small heterocyclic P3 caps in HCV NS3 protease inhibitors. N. Sin, B. L. Venables, L. Sun, A. X. Wang, S. Sit, Y. Chen, J. Chen, Y. Han, A. C. Good, J. Friborg, D. Barry, F. Yu, D. Hernandez, A. Sheaffer, J. Knipe, F. McPhee, N. A. Meanwell, P. M. Scola 123. Cyclic phosphate prodrugs of 2�deoxy-2�-fluoro-2�-C-methyl nucleoside analogs as inhibitors of HCV NS5B polymerase. P. Reddy, D. Bao, W. Chang, B. Chun, J. Du, D. Nagarathnam, S. Rachakonda, B. S. Ross, H. Zhang, S. Bansal, C. L. Espiritu, M. Keilman, A. M. Lam, C. Niu, H. M. Steuer, P. A. Furman, M. J. Otto, M. J. Sofia 124. Discovery of PSI-353661: A novel purine nucleotide prodrug with improved in vitro potency for the treatment of HCV infection. W. Chang, D. Bao, B. Chun, D. Nagarathnam, S. Rachakonda, P. Reddy, B. S. Ross, H. Zhang, S. Bansal, C. L. Espiritu, M. Keilman, A. M. Lam, C. Niu, H. M. Steuer, P. A. Furman, M. J. Otto, M. J. Sofia 125. Synthesis of novel, fluorinated P1 NS3 protease inhibitors of HCV. Y. Chen, S. Sit, J. Chen, L. Sun, S. V. D’Andrea, Z. Zheng, A. X. Wang, S. Hiebert, M. Bowsher, A. Cocuzza, Q. Zhao, D. Bilder, N. Sin, B. L. Venables, D. Carini, B. Johnson, E. Mull, D. Hernandez, A. K. Sheaffer, H. Mulherin, F. Yu, J. O. Knipe, K. Mosure, A. C. Good, R. Rajamani, H. Klei, J. Friborg, V. Arora, Y. Shu, X. Huang, L. Levesque, D. Li, J. Zhu, S. Adam, F. McPhee, N. Meanwell, P. M. Scola 126. Synthesis and SAR studies on highly potent, novel, N,1-C2- phenyl-bridged 2-phenyl-indole-6-carboxamide based hepatitis C virus NS5B inhibitors. X. Zheng, T. W. Hudyma, M. Ding, F. He, M. A. Poss, J. F. Kadow, C. Chang, c. wan, M. R. Witmer, P. Morin, D. M. Camac, S. Sheriff, B. R. Beno, K. Rigat, Y. Wang, R. Fridell, J. Lemm, D. Qiu, P. Liu, S. Voss, S. B. Roberts, M. Gao, J. Knipe, R. G. Gentles 127. Isoquinoline tripeptides as HCV NS3 protease inhibitors. Z. B. Zheng, A. X. Wang, D. Carini, A. Cocuzza, S. Hiebert, M. Bowsher, Y. Chen, S. Sit, L. Sun, F. Mcphee, J. Friborg, D. Barry, F. Yu, D. Hernandez, J. Knipe, R. Rajaman, H. Klei, A. Ng, B. Ma, Q. Gao, N. A. Meanwell, P. M. Scola, S. D’Andrea 128. SAR and mode of binding studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamides: Potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus. R. G. Gentles, M. Ding, X. Zheng, L. Chupak, M. A. Poss, C. Chang, C. Wan, M. R. Witmer, P. Morin, D. M. Camac, S. Sheriff, B. R. Beno, K. Rigat, S. B. Roberts, M. Gao, J. F. Kadow, J. Lemm, S. Voss, M. Liu, L. Pelosi, Y. Wang 129. Development of novel carbohydrate binding agents: A new class of potent antiviral therapeutics. P. C. Trippier, J. Balzarini, C. McGuigan 130. Synthesis and HIV-1 integrase inhibitory activity of C2-C-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides. B. Naidu, M. E. Sorenson, M. Patel, Y. Ueda, J. Banville, F. Beaulieu, S. Bollini, I. Dicker, H. Higley, Z. Lin, L. Pajor, D. D. Parker, B. Terry, M. Zheng, A. Martel, N. A. Meanwell, M. Krystal, M. A. Walker 131. Design, synthesis and HIV-1 integrase inhibitory activity associated with spirocycle-fused5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides. B. Naidu, M. E. Sorenson, J. D. Matiskella, Y. Ueda, S. Bollini, I. Dicker, H. Higley, Z. Lin, D. Wu, L. Pajor, D. D. Parker, B. Terry, M. Zheng, N. A. Meanwell, M. Krystal, M. A. Walker 132. Synthesis and evaluation of novel phosphoramidates of acyclic nucleosides in the bypass of the first phosphorylation step mediated by the thymidine kinase. D. Carta, C. McGuigan, C. Vanpouille, L. Margolis, J. Balzarini 133. Study of C2-N-linked heterocyclic pyrimidin-6-oxa-5-hydroxy-4-carboxamide derivatives as HIV integrase inhibitors. M. Sorenson, B. Naidu, J. Matiskella, T. Connolly, Y. Ueda, N. Meanwell, S. Bollini, H. Samanta, B. Terry, Z. Lin, I. Dicker, D. Parker, L. Pajor, M. Zheng, M. Krystal, M. Walker 134. Design, synthesis and SAR study of novel spiro aza-pyrimidinone HIV integrase inhibitors. c. li, M. A. Walker, Y. Ueda, J. Matiskella, Z. Lin, I. Dicker, H. Samanta, B. Terry, H. Higley, S. Bollini, M. Krystal, N. A. Meanwell 135. Discovery and preclinical evaluation of the HIV integrase inhibitor BMS-727740. M. A. Walker, J. Banville, B. Naidu, M. Sorenson, R. Remillard, A. Martel, Y. Ueda, T. Connolly, J. Weiss, C. Li, A. Trehan, H. Wong, Z. Lin, I. Dicker, H. Samanta, B. Terry, H. Scarnati, C. Deminie, S. Bollini, M. Zheng, A. Chimalakonda, L. Pajor, T. Philip, D. Parker, M. Krystal, N. A. Meanwell 136. Towards the synthesis of novel boronates as potential HIV-1 protease inhibitors. J. L. Nye, D. R. Clayton, M. S. McCammant, L. Fabry-Asztalos 137. Novel spirocyclobutyl- and spirocyclooxetanyl-pyrimidin-6-oxa-5-hydroxy- 4-carboxybenzylamides as potent HIV-1 integrase inhibitors. T. P. Connolly, I. Dicker, M. Krystal, Z. Lin, J. Matiskella, N. A. Meanwell, B. Naidu, L. Pajor, M. Sorenson, B. Terry, Y. Ueda, M. A. Walker, M. Zheng 138. Design, synthesis and structure-activity relationships of novel dicamphanoyl- 2�,2�-dimethyldihydropyranochromone (DCP) analogs as potent anti-HIV agents. T. Zhou, C. Chen, Q. Shi, L. Huang, P. Ho, K. Lee 139. HIV-1 protease inhibitors with a tertiaryalcohol-containing transition-state mimic and various P2/P1� substituents. P. Öhrngren, X. Wu, J. K. Ekegren, T. Unge, &. Rosenquist, B. Samuelsson, M. Larhed 140. Design and synthesis of novel isatin derivatives as potent anti-HIV agents. R. K. Singh, G. Kumari, M. Yadav 141. Small molecules to target Mycobacterium tuberculosis 1-Deoxy-D-xylulose-5phosphate reducto-isomerase (MtbDxr). E. R. Jackson, K. Kehn-Hall, F. Kashanchi, H. I. Boshoff, C. S. Dowd 142. Synthesis and in silico studies of altered DNA substrates as HIV RT inhibitors. M. Yadav, G. Kumari, R. K. Singh 143. Synthesis of new antimalarial bi-drug molecules. A. Jonet, A. Dassonville-Klimpt, P. Sonnet 144. Motualevic acid analogs: Synthesis, antimicrobial activity, and structure�activity relationship (SAR) studies. P. Cheruku, J. L. Keffer, C. A. Bewley 145. New bicyclic peptidomimetic inhibitors of secreted aspartic proteinase 2 (SAP2) for the treatment of drug-resistant Candida albicans infections. A. Trabocchi, C. Calugi, A. Cassone, R. Cauda, A. Guarna 146. Quinolonimines as novel antimalarial leads. T. Rodrigues, J. Gut, P. J. Rosenthal, R. Moreira, R. Guedes, D. Santos, F. Lopes 147. Discovery and development of the covalent hydrates of trifluoromethylated pyrazoles as riboflavin synthase inhibitors with antitubercular activity. A. Talukdar, A. Bacher, B. Illarionov, M. Fischer, S. G. Franzblau, B. Wan, M. Cushman 148. Hybrid compounds targeting both liver and blood stages of malaria parasites. F. Lopes, R. Capela, R. Moreira, P. J. Rosenthal, J. Gut, G. Cabal, M. Prudêncio, M. Mota 149. Synthesis and antiviral activity of a second generation of measles virus RNA-dependent RNA polymerase activity inhibitors. J. M. Ndungu, S. A. Krumm, A. Sun, R. K. Plemper, J. P. Snyder 150. Design and synthesis of a sixteen million member DNA-encoded library (DEL) and discovery of potent Mycobacterium tuberculosis (Mtb) InhA inhibitors. C. P. Davie, P. A. Centrella, G. K. O’Donovan, G. Evindar, H. O’Keefe, A. M. Patel, M. A. Clark 151. Cell-based optimization of imidazolopiperazines as new antimalarials. T. Wu, A. Nagle, K. Kuhen, K. Henson, R. Borboa, C. Francek, Z. Chen, D. Plouffe, J. Chang, C. Li, T. Tuntland, J. Isbell, M. Rottmann, E. Winzeler, R. Glynne, D. C. Tully, A. K. Chatterjee 152. Modeling trypanosomal TOR kinase domains: Implications for the design of antiparasitic drugs. Z. Wang, C. E. Hubbard, M. Ondrechen, M. P. Pollastri 153. High-speed synthesis of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines applied to bone morphogenetic protein signaling inhibitors. J. Liu,G.D.Cuny,P.B.Yu, X. Xing, K. D. Bloch, R. T. Peterson 154. Total synthesis of YM-181741 for the preparation of natural product-like STAT3:STAT3 inhibitors. A. Misale, D. Antonow, D. E. Thurston, G. Zinzalla 155. Tetrapodal Stat3 inhibitors offer potent disruption of Stat3 in vitro and in whole cell assays. B. D. Page, A. Schimmer, J. Turkson, P. T. Gunning 156. NO-NSAIDs: Nitric oxide-releasing prodrugs of non-steroidal anti-inflammatory drugs with gastric-sparing properties. K. V. Nemmani, N. Borhade, A. R. Pathan, S. V. Mali, M. Karwa, S. S. P., V. Pamidiboina, M. Gund, N. J. Deshmukh, P. Gaikwad, A. K. Jain, J. J. Deshattiwar, S. Halder, D. C. Desai, J. Mudgal, M. Dhiman, A. U. Burhan, A. Sharma, N. P. Dubash, N. K. Mangu, M. Dutta, G. Thakre, S. Goud, D. Pacharne, L. Babu, S. Deshpande, V. Nadar, S. Sharma, A. Satyam 157. Inhibition of CuZnSOD by low MW natural products. J. S. Summers, M. E. Arrington, M. R. Yost, J. Markley, E. Parris, B. Hickman, J. Schmitt 158. Thiobenzimidazole-1-acetic acids as CRTH2 antagonists. J. Pothier, A. Fecher, M. Gude, K. Hilpert, M. A. Riederer, X. Leroy, O. Peter, H. Kletzl, C. Gnerre, R. Bravo, S. Delahaye, L. Piali, F. Sylvie, H. Fretz 159. Development of SH2 domain proteomimetics as potent disruptors of oncogenic Stat3:Stat3 dimerization. J. A. Drewry, P. T. Gunning 160. 1,3,6-substituted-4-aminopyrazolopyrimidines, new potent inhibitors for phopholipase D. J. Baffoe, A. M. Kulkarni, V. Curry, B. Török, K. Stieglitz 161. Development of potent and selective MMP inhibitors with a triazole zinc binding group. J. Haas,A.M.Fryer, S. W. Andrews, L. Huang, J. A. Josey, S. Kragerud, Y. Marsh, J. P. Rizzi, F. Sullivan 162. Reduction of hERG activity in (4,5,6,7tetrahydro-1H-indazolyl)ethanamines, a novel series of potent and selective S1P1 selective agonists. N. Aguilar, M. Carrascal, M. Erra, S. Fonquerna, L. Taboada, J. Alonso, B. Vidal, N. Godessart, G. Tarrasón, T. Domenech, C. Armengol, M. Córdoba, M. Sabaté, D. Casals, M. Domínguez 163. Structure-activity relationship studies of sphingosine kinase inhibitors. M. R. Raje, Y. Kharel, K. R. Lynch, W. L. Santos 164. Amido-1,3,4-thiadiazole derivatives as novel S1P1 selective agonists: From an HTS hit to a sub-nanomolar, orally active advanced lead. N. Aguilar, M. Mir, P. Grima, M. López, N. Godessart, G. Tarrasón, T. Domenech, D. Vilella, C. Armengol, M. Córdoba, M. Sabaté, D. Casals, M. Domínguez 165. Structure-based design of potent, conformationally constrained, cell-permeable STAT3 inhibitors. J. Chen,L.Bai, Y. Zhao, D. Bernard, Z. Nikolovska-Coleska, C. Gomez, J. Zhang, H. Yi, S. Wang 166. Structure and activity relationships of tartrate-based TACE inhibitors. D. Li, J. V. Popovici-Muller, D. B. Belanger, J. Caldwell, C. Dai, M. David, V. M. Girijavallabhan, Z. Guo, J. A. Kozlowski, B. J. Lavey, D. J. Lundell, J. F. Lee, Z. Liu, R. Mazzola, B. McKittrick, X. Niu, P. Orth, V. Madison, J. Piwinski, R. Rizvi, K. E. Rosner, B. Shankar, N. Shih, G. W. Shipps, M. Siddiqui, J. Spitler, C. O. Strickland, J. Sun, P. C. Ting, S. Chen, H. Vaccaro, W. Yu, G. Zhou, Z. Zhu 167. New nNOS PDZ domain ligands and their biological evaluation. A. M. Perez-Lopez, J. M. Cardenas-Maestre, R. Salto-Gonzalez, M. Giron-Gonzalez, J. Martinez-Lopez, T. de la Rubia-Nieto, J. F. Dominguez-Seglar, R. Sanchez-Martin, J. A. Gomez-Vidal 168. Synthesis of a series of nonpeptidic thiochromanone-based thiosemicarbazone analogs as inhibitors of cathepsin L. J. Song, L. M. Jones, K. Gaddale Devanna, E. S. Conner, G. E. Chavarria, A. K. Charlton-Sevcik, M. L. Trawick, B. G. Siim, D. J. Chaplin, K. G. Pinney 169. Thiosemicarbazone derivatives of functionalized tetralone, indanone, chromanone, and 2,3-dihydroquinolinone scaffolds as inhibitors of cathepsins L and B. L. M. Jones,J.Song, A. L. Johansen, A. K. Jantz, G. E. Chavarria, A. K. Charlton-Sevcik, M. Trawick, B. G. Siim, D. J. Chaplin, K. G. Pinney 170. Rigidified 2-aminopyrimidines as histamine H 4 receptor antagonists: Effects of substitution about the rigidifying ring. J. R. Koenig, H. Liu, I. Drizin, D. G. Witte, T. L. Carr, A. M. Manelli, I. Milicic, M. I. Strakhova, T. R. Miller, T. A. Esbenshade, J. D. Brioni, M. Cowart 171. Design and synthesis of 3-alkylsulfonylmethylcyclohexylaminobenzamide-derived inhibitors of CC chemokine receptor 2 (CCR2). M. G. Yang,D.G.Batt, R. J. Cherney, S. Mandlekar, M. Cvijic, Q. Zhao, J. C. Barrish, P. H. Carter The official technical program for the 240th National Meeting is available at: www.acs.org/boston2010 MEDI TECH–75
MEDI TECHNICAL PROGRAM 172. Synthesis and development of multimeric molecules to mimic the pro-apoptotic ligand TRAIL, a member of the TNF superfamily. M. Lechner, J. Beyrath, V. Pavet, C. Pardin, A. Morizot, M. Wendland, W. Maison, O. Micheau, H. Gronemeyer, S. Fournel, G. Guichard 173. Utilizing a pharmacophore model for the development of potent small molecule inhibitors of STAT3 function. V. M. Shahani, S. Fletcher, P. Yue, D. P. Luu, S. Sharmeen, A. D. Schimmer, J. Turkson, P. T. Gunning* 174. Design and synthesis of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of members of the CLK and DYRK kinase families. A. S. Rosenthal, C. Tanega, M. Shen, B. T. Mott, D. S. Auld, J. Inglese, C. P. Austin, D. J. Maloney, C. J. Thomas 175. Design, synthesis and structure-activity relationships of potent B-RAF inhibitors. N. Namdev, J. Lapierre, Y. Liu, H. Wu, C. Brassard, N. Westlund, M. Tandon, J. Link, D. Kizer, R. Nicewonger, K. Bresciano, T. Hall, J. Szwaya, C. Chen, D. France, M. A. Ashwell 176. Discovery of pyrazol-3-yl and thiazol- 2-yl amino pyrazines as novel JAK2 inhibitors. L. Almeida, S. Ioannidis, M. L. Lamb, A. M. Davies, M. Su, B. Peng, H. Guan, G. Bebernitz, M. Ye, K. Bell, M. Alimzhanov, M. Zinda 177. Utilization of 1,3,5-triazine as a pyrimidine surrogate for the evaluation of PDK1 inhibitors. M. Bobko, K. Evans, J. Axten, J. Medina, L. Shuster, C. Blackledge, S. Grant, A. Shu, C. Becker, S. Rabindran, C. Gardiner, H. Xiang 178. Design, synthesis and biological evaluation of novel quinoxaline derivatives as PI3K inhibitors. P. Wu, Y. Su, L. Zhang, S. Y. Wen, J. C. Xu, B. Yang, Q. J. He, Y. Z. Hu 179. Structure-based discovery and optimization of a novel protein kinase B (AKT) inhibitor. F. Lopez-Vallejo, A. Hernandez-Campos, I. Velazquez-Martinez, R. Castillo, Y. Yu, N. Singh, M. Giulianotti, J. Medina-Franco 180. Design and synthesis of a novel, potent, and selective class of type II p38 inhibitors. D. V. Nguyen, R. Shetty, N. Jayasuriya, E. L. Michelotti, F. Machrouhi, J. Gaboury, W. Evans, H. V. Namboodiri, M. Bukhtiyarova, S. Mardirosian, M. Guo, T. Fujimoto 181. Development of a gene family targeted workflow for the identification of inhibitors of kinase targets. P. D. Kane, J. A. Foster, R. J. Foster, J. Swanson, M. S. Lawless 182. Novel approaches to CDK2 modulation: Hit identification, characterization, and optimization. Y. Deng, G. W. Shipps, P. J. Curran, L. Zhao, M. A. Siddiqui, J. Popovici-Muller, J. S. Duca, A. W. Hruza, T. O. Fischmann, V. S. Madison, R. Zhang, C. W. McNemar, T. W. Mayhood, E. M. Lees, D. A. Parry, W. T. Windsor 183. Design, synthesis and in vitro characterization of phosphate pro-drugs of mutant-B-RAF inhibitors. Y. Liu, J. Lapierre, M. Tandon, N. Namdev, H. Wu, C. Brassard, E. Volckova, J. Szwaya, C. Chen, D. France, M. A. Ashwell 184. Design and synthesis of 4-subtituted thiazoles as AKT inhibitors. X. Wang, Q. Zeng, M. Bourbeau, M. Lee, G. Yao, S. Tadesse, F. Hong, C. Yuan, X. Huang, B. Han, E. Wohlhieter, J. Allen, S. Zhang, J. Lofgren, X. Zhang, D. Freeman, J. Bready, C. Davis, C. Fotsch, R. Hungate, R. Kendall 185. Design and synthesis of novel heterocyclic scaffolds as protein kinase inhibitor. L. Wei, S. V. Malhotra 76–TECH ‡ Cooperative Cosponsorship 186. Discovery of orally bioavailable Aurora kinase inhibitors. D. B. Belanger, M. J. Williams, Z. Meng, T. Yu, A. K. Mandal, P. J. Curran, M. P. Rainka, N. Shih, M. A. Siddiqui, A. D. Basso, D. Prelusky, M. Liu, S. Lee, B. Yaremko, K. Gray, S. Tevar, J. Jones, E. B. Smith 187. Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38� MAP kinase inhibitors. A. J. Dyckman, T. Li, G. Schieven, S. Pitt, R. Zhang, D. Shen, M. McKinnon, K. McIntyre, K. Gillooly, D. Shuster, A. Doweyko, J. Sack, H. Zhang, P. Marathe, J. Barrish, J. Dodd, K. Leftheris 188. Discovery of 2-aminophenyl quinazolines as potent and selective PDK1 inhibitors. X. Lin, M. Aikawa, P. Amiri, S. Basham, J. Chan, R. Jain, S. Lin, T. Machajewsky, W. McCrea, D. Menezes, J. Murray, S. Ng, K. Pfister, A. C. Rico, S. Ramurthy, W. Shu, S. Subramanian, J. Sutton, E. Venetsanakos, M. X. Wang, B. Warne, Y. Xu, R. Zang, Y. Zhou 189. SAR of a new series of Stearoyl-CoA desaturase inhibitors. J. Leclerc, C. Chan, J. Falgueyret, J. Guay, S. Guiral, Z. Huang, N. Lachance, C. Li, R. Oballa, Y. K. Ramtohul, L. Zhang 190. Synthesis of pyrazolospiroketone ACC inhibitors. C. Limberakis, S. Bader, L. M. Buzon, S. B. Coffey, B. G. Conway, J. W. Corbett, K. D. Freeman-Cook, K. E. Henegar, C. S. Jones, K. L. Nelson, W. Song, J. D. Weaver, Z. Zhao, D. P. Phillion 191. Discovery of a potent small molecule inhibitor of IGF-1R. D. Frennesson, M. Wittman, M. Saulnier, J. Carboni, R. Attar, P. Balimane, C. Chang, C. Chen, L. Discenza, M. Gottardis, A. Greer, W. Hurlburt, W. Johnson, D. Langley, F. Lee, A. Li, P. Liu, H. Mastalerz, A. Mathur, K. Menard, K. Patel, J. Sack, X. Sang, S. Traeger, G. Trainor, U. Velaparthi, Z. Yang, G. Zhang, K. Zimmermann, D. Vyas 192. Novel dual agonists of the GPR40 and PPAR� receptors. E. Marsault, H. Tremblay, F. Chagnon, A. Beauregard, A. Émond, P. Boulais, M. Langlois, R. Leduc 193. Novel cambinol analogs as sirtuin inhibitors: Synthesis, biological evaluation and rationalisation of activity. F. Medda, L. Pirrie, S. Poupart, R. J. Russell, M. Higgins, A. R. McCarthy, J. Campbell, A. M. Slawin, D. P. Lane, S. Lain, N. J. Westwood 194. Metabolism-guided design of amino alcohol acids as orally active, short-acting calcium-sensing receptor antagonists. G. Balan, Y. Zhang,J.N.Bauman, T. A. Brown, G. Fate, D. R. Healy, M. Herr, P. Humphries, A. S. Kalgutkar, B. Kapinos, M. Li, T. S. Maurer, C. Neagu, R. Oliver, V. M. Paralkar, D. A. Price, K. A. Riccardi, J. Sagal, J. A. Southers, S. Spath, I. A. Stock 195. Synthesis of possible calcimimetic derivatives from enantiopure primary amines. S. Espinosa-Diaz, J. L. Alvarez, K. M. Santiago 196. Discovery of TAK-875: A potent, selective, and orally bioavailable GPR40 agonist. N. Negoro, S. Sasaki, S. Mikami, M. Ito, M. Suzuki, Y. Tsujihata, R. Ito, A. Harada, K. Takeuchi, N. Suzuki, J. Miyazaki, T. Santou, N. Kanzaki, S. Satou, T. Odani, J. Sakamoto, M. Funami, T. Tanaka, A. Kogame, S. Matsunaga, T. Yasuma, Y. Momose 197. Investigation of functionally liver selective glucokinase activators. H. F. Schuster,L.C.Kirman, G. R. Bebernitz, M. S. Grondine, A. Duttaroy, S. L. Caplan, P. M. Taslimi, B. A. Dale, J. Gao, R. Deacon, V. Beaulieu, W. M. Maniara, T. Stams, B. Vash, R. C. Gupta, S. Munshi, S. S. Nadkarni 198. Glucokinase activators with improved physicochemical properties and off target effects. L. C. Kirman, H. F. Schuster, M. S. Grondine, G. R. Bebernitz, S. L. Caplan, A. Duttaroy, P. M. Taslimi, B. A. Dale, J. Gao, J. Liang, V. Beaulieu, R. Deacon 199. Investigation of chiral sulfoxide GPR119 agonists for type 2 diabetes. G. E. Peckham 200. Rearrangement of the SSTR5 agonist L-817,818 under physiological conditions affords an alternate SSTR5 agonist that elevates plasma glucose excursion during OGTT. M. Reiter, J. Terebetski, D. Shen, B. Murphy, J. L. Duffy 201. Design, synthesis and evaluation of novel (4-piperidinyl)-piperazine class as acetyl-CoA carboxylase 1/2 non-selective inhibitors. T. Chonan, D. Wakasugi, D. Yamamoto, M. Yashiro, T. Oi, H. Tanaka, A. Ohoka-Sugita, F. Io, H. Koretsune, A. Hiratate 202. Discovery of O-spiroketal C-arylglucosides as novel and selective sodiumdependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. T. Sato, T. Kobayashi, M. Nishimoto, N. Taka, Y. Ohtake, K. Takano, K. Yamamoto, M. Ohmori, M. Yamaguchi, K. Takami, S. Yeu, K. Ahn, H. Matsuoka, M. Suzuki, H. Hagita, K. Ozawa, K. Yamaguchi, M. Kato, S. Ikeda 203. Synthesis and evaluation of a series of piperazinylpyridines as GPR119 agonists. Y. Wu, J. D. Kuntz, A. Carpenter 204. Structure-based Virtual Screening for the discovery of potential P2Y14 receptor ligands. F. Deflorian, A. Szabo, K. A. Jacobson 205. Exploring structural scaffolds as a strategy to design selective ligands. A. B. Yongye, Y. Li, M. A. Giulianotti, Y. Yu, R. A. Houghten, A. Nefzi, L. Chaker, K. Martinez-Mayorga 206. Optimization of phenylmethylene hydantoins as prostate cancer migration inhibitors: SAR-directed design, synthesis, and pharmacophore modeling. M. Mudit, K. A. El Sayed 207. Art of crystallization and application of single crystal X-ray diffraction to support solid-state characterization of pharmaceuticals. N. Tsou, A. Mckeown, R. Ball, M. McNevin, C. Maguire, A. Chen, A. Bak 208. Estrogen receptor antagonist-functionalized gold nanoparticles for breast cancer drug delivery and imaging systems. K. D. Dao, R. N. Hanson, R. Sawant, V. Torchilin 209. Bipolar biphenyl proteomimetics as estrogen receptor � and androgen receptor coactivator binding inhibitors. P. T. Weiser, A. B. Williams, R. N. Hanson 210. Identification of a novel series of [2.2.1]oxabicyclo lactam-based androgen receptor antagonists. J. F. Austin, L. S. Sharma, A. J. Balog, W. Shan, A. J. Nation, D. S. Nirschl, A. V. Miller III, G. D. Vite, C. A. Rizzo, M. Gottardis, J. Dell-John, L. Zhang, R. Attar, L. Schweizer, M. T. Obermeier, M. N. Jure-Kunkel, T. E. Spires, A. V. Gavai 211. Development and application of the pharmacophore model of pregnane X receptor. J. Ramanjulu, A. S. Lakdawala, S. Williams, R. Marquis 212. Synthesis and evaluation of fluorinated �1-adrenoreceptor selective ligands. H. S. Radeke, A. Purohit, T. D. Harris, K. Hanson, M. Broekema, C. Hu, R. Jones, M. Azure, M. Cdebaca, P. Yalamanchili, M. Kavosi, M. Yu, M. Guaraldi, J. McDonald, M. Kagan, S. Robinson, D. Casebier 213. Tetra-aryl cyclobutanes as direct inhibitors of the nuclear receptor/coactivator interaction. A. A. Parent, J. R. Gunther, J. A. Katzenellenbogen 214. Identification of allosteric potentiators of the prostaglandin receptor EP2. T. Ganesh,J.Jiang,Y.Du,R.Shaw, P. Thepchatri, R. Dingledine 215. Design, synthesis, and evaluation of isoquinoline urea derivatives of A-425619 as TRPV1 antagonists. N. A. Gujarati, B. J. Undem, V. L. Korlipara 216. Conformationally constrained analogs of BAY 59-3074, a CB1 cannabinoid receptor partial agonist. H. Teng, G. Thakur, A. Makriyannis 217. Arylguanidines as analgesic adjuvants: Graphics modeling studies. G. S. Alley, P. D. Mosier, M. Dukat 218. Novel peptidyl boronic acid based inhibitors of PSA. M. B. Kostova, D. M. Rosen, S. R. Denmead 219. Amino aryl sulfonamides as novel and potent 5-ht 6 receptor ligands. R. Nirogi, R. Kambhampati, T. Bandyala, J. Konda, S. Arepalli, V. Reballi, P. Kothmirkar, N. Pamuleti, A. Shinde 220. Strategy for conjugation of “clickable” agonists of the A 3 adenosine receptor to polyamidoamine (PAMAM) dendrimers. D. K. Tosh,L.S.Yoo,M.Chinn,Z.Gao, K. A. Jacobson 221. Structure-activity relationship of (N)methanocarba phosphonate analogs of 5�-AMP as cardioprotective agents acting through a cardiac P2X receptor. S. Thatikonda, S. Zhou, B. V. Joshi, R. Balasubramanian, T. Yang, B. T. Liang, K. A. Jacobson 222. Chemical enhancement for skin drug delivery using gemini surfactants. S. Silva, J. Sousa, A. Pais, B. Michniak-Kohn 223. Development of small molecular weight non-aminoglucosides for compound-induced readthrough of premature termination codons caused by nonsense mutations. J. Ku, L. Du, R. Damoiseaux, H. Hu, C. Bertoni, R. A. Gatti, M. E. Jung 224. Characterizations of diastereoisomers of polyamine analogs with oxime functionalites. H. Shin, E. Rawls, H. Whitehead, J. Lee, S. Kim 225. Development and evaluation of a novel radiogallium labeled peptide as a bone imaging agent for PET. K. Ogawa, K. Takai, T. Kiwada, Y. Kitamura, K. Shiba, A. Odani 226. Fluorescence-labeled celecoxib derivatives as novel pharmacological tools. A. P. Lill, S. Schiffmann, S. Groesch, E. Proschak, H. Stark 227. Design and optimization of a potent series of eIF4E inhibitors. D. Kopecky, X. Chen, J. Mihalic, J. Heath, J. Deignan, F. Kayser, S. Jeffries, Z. Wang, S. Johnstone, X. Min, M. Cardozo, S. Shen, M. Lo 228. Discovery of a pyrimidinone-based antagonist of calcium sensing receptor. J. Ramanjulu, L. Casillas, A. Charnley, M. DeMartino, X. Dong, P. Harris, J. Jeong, Y. Lan, A. Rahman, L. Dare, M. Schaeffer, S. Hoffman, S. Kumar, R. Marquis 229. Dimeric modulators of ENaC for the treatment of cystic fibrosis. U. Baettig, R. Butler, N. Smith, E. Stanley, P. Oakley, S. Collingwood, H. Danahay, K. Coote, H. Atherton, D. Paisley, R. Lock 230. Conformationally constrained peptides as the Src SH3 domain binding ligands. R. Tiwari, A. Brown, S. Narramaneni, G. Sun, K. Parang 231. Discovery of novel 4-oxo-2-thioxo-7quinazoline carboxamides and derivatives as prolyl hydroxylase inhibitors. M. J. Schulz,G.L.Adams, J. A. Brackley, H. Yu, J. M. Ghergurovich, R. M. Sanchez, J. Qu, G. Burton, Y. Wang Photographing or recording meeting sessions and/or activities other than your own are prohibited at all official ACS events without written consent from ACS.
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