In This Issue

In This Issue, Volume 4, Issue 6 Janice Elaine Y. Silverman 497-497 Full: PDF (792 K)

Patent Highlights

Imidazopyrazine Derivatives As Inhibitors of mTOR Gerard Rosse 498-499 Full: PDF (253 K)

Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype Gerard Rosse 500-501 Full: PDF (221 K)

Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down’s Syndrome or Alzheimer’s Disease Gerard Rosse 502-503 Full: PDF (414 K)

Letters

Identification of New Nonsteroidal RORα Ligands; Related Structure–Activity Relationships and Docking Studies Mathieu Dubernet, Nicolas Duguet, Lionel Colliandre, Christophe Berini, Stéphane Helleboid, Marilyne Bourotte, Matthieu Daillet, Lucie Maingot, Sébastien Daix, Jean-François Delhomel, Luc Morin-Allory, Sylvain Routier, and Robert Walczak 504-508 Full: PDF (1492 K)

Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase Ping Liu, Terence G. Hamill, Marc Chioda, Harry Chobanian, Selena Fung, Yan Guo, Linda Chang, Raman Bakshi, Qingmei Hong, James Dellureficio, Linus S. Lin, Catherine Abbadie, Jessica Alexander, Hong Jin, Suzanne Mandala, Lin-Lin Shiao, Wenping Li, Sandra Sanabria, David Williams, Zhizhen Zeng, Richard Hajdu, Nina Jochnowitz, Mark Rosenbach, Bindhu Karanam, Maria Madeira, Gino Salituro, Joyce Powell, Ling Xu, Jenna L. Terebetski, Joseph F. Leone, Patricia Miller, Jacquelynn Cook, Marie Holahan, Aniket Joshi, Stacey O’Malley, Mona Purcell, Diane Posavec, Tsing-Bau Chen, Kerry Riffel, Mangay Williams, Richard Hargreaves, Kathleen A. Sullivan, Ravi P. Nargund, and Robert J. DeVita 509-513 Full: PDF (1190 K)

Metabolically Stable tert-Butyl Replacement David Barnes-Seeman, Monish Jain, Leslie Bell, Suzie Ferreira, Scott Cohen, Xiao-Hui Chen, Jakal Amin, Brad Snodgrass, and Panos Hatsis 514-516 Full: PDF (388 K)

SAR-Based Optimization of a 4-Quinoline Carboxylic Acid Analogue with Potent Antiviral Activity Priyabrata Das, Xiaoyi Deng, Liang Zhang, Michael G. Roth, Beatriz M. A. Fontoura, Margaret A. Phillips, and Jef K. De Brabander 517-521 Full: PDF (729 K)

Enzymatic Stability and Immunoregulatory Efficacy of a Synthetic Indolicidin Analogue with Regular Enantiomeric Sequence Ching-Yun Chang, Chih-Wei Lin, Sheng-Kuo Chiang, Po-Ling Chen, Chiung-Yi Huang, Shih-Jen Liu, Pele Chong, and Ming-Hsi Huang 522-526 Full: PDF (1278 K)

Development of Unsymmetrical Dyads As Potent Noncarbohydrate-Based Inhibitors against Human β-N-Acetyl-d-hexosaminidase Peng Guo, Qi Chen, Tian Liu, Lin Xu, Qing Yang, and Xuhong Qian 527-531 Full: PDF (1792 K)

Identification of Selective Nanomolar Inhibitors of the Human Neuraminidase, NEU4 Amgad Albohy, Yi Zhang, Victoria Smutova, Alexey V. Pshezhetsky, and Christopher W. Cairo 532-537 Full: PDF (2674 K)

New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi Laura Friggeri, Luigi Scipione, Roberta Costi, Marcel Kaiser, Francesca Moraca, Claudio Zamperini, Bruno Botta, Roberto Di Santo, Daniela De Vita, Reto Brun, and Silvano Tortorella 538-541 Full: PDF (1095 K)

Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase Baisong Zheng, Yuan Yao, Zhen Liu, Lisheng Deng, Justin L. Anglin, Hong Jiang, B. V. Venkataram Prasad, and Yongcheng Song 542-546 Full: PDF (1659 K)

3-Hydroxyquinolin-2(1H)-ones As Inhibitors of Influenza A Endonuclease Hye Yeon Sagong, Ajit Parhi, Joseph D. Bauman, Disha Patel, R. S. K. Vijayan, Kalyan Das, Eddy Arnold, and Edmond J. LaVoie 547-550 Full: PDF (2173 K)

Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles Yingcai Wang, Jiwen (Jim) Liu, Paul J. Dransfield, Liusheng Zhu, Zhongyu Wang, Xiaohui Du, Xianyun Jiao, Yongli Su, An-rong Li, Sean P. Brown, Annie Kasparian, Marc Vimolratana, Ming Yu, Vatee Pattaropong, Jonathan B. Houze, Gayathri Swaminath, Thanhvien Tran, Khanh Nguyen, Qi Guo, Jane Zhang, Run Zhuang, Frank Li, Lynn Miao, Michael D. Bartberger, Tiffany L. Correll, David Chow, Simon Wong, Jian Luo, Daniel C.-H. Lin, and Julio C. Medina 551-555 Full: PDF (1238 K)

New Peptide-Based Antimicrobials for Tackling Drug Resistance in Bacteria: Single-Cell Fluorescence Imaging Jean-Marie Pagès, Slavka Kascàkovà, Laure Maigre, Anas Allam, Mickael Alimi, Jacqueline Chevalier, Erwan Galardon, Matthieu Réfrégiers, and Isabelle Artaud 556-559 Full: PDF (645 K)

Discovery of a Potent, Dual Serotonin and Norepinephrine Reuptake Inhibitor Nicolas Dreyfus, Jason K. Myers, Valentina O. Badescu, Oscar de Frutos, Maria Luz de la Puente, Chunjin Ding, Sandra A. Filla, Karsten Fynboe, Douglas L. Gernert, Beverly A. Heinz, Susan K. Hemrick-Luecke, Kirk W. Johnson, Michael P. Johnson, Pilar López, Patrick L. Love, Laura J. Martin, Thierry Masquelin, Michael J. McCoy, Javier Mendiola, Denise Morrow, Mark Muhlhauser, Gustavo Pascual, Thomas J. Perun, Lance A. Pfeifer, Lee A. Phebus, Simon J. Richards, Juan Antonio Rincón, Eric P. Seest, Jikesh Shah, Jia Shaojuan, Rosa Maria A. Simmons, Gregory A. Stephenson, Eric G. Tromiczak, Linda K. Thompson, Magnus W. Walter, Wayne W. Weber, Hamideh Zarrinmayeh, Craig E. Thomas, Elizabeth Joshi, Smriti Iyengar, and Anette M. Johansson 560-564 Full: PDF (886 K)

Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold Mattia Mori, Assunta Massaro, Vito Calderone, Marco Fragai, Claudio Luchinat, and Alessandro Mordini 565-569 Full: PDF (2511 K)