Search Results - "MACIELAG, Mark J"

Pharmacologic Characterization of JNJ-42226314, [1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a Reversible, Selective, and Potent Monoacylglycerol Lipase Inhibitor by Wyatt, Ryan M, Fraser, Ian, Welty, Natalie, Lord, Brian, Wennerholm, Michelle, Sutton, Steven, Ameriks, Michael K, Dugovic, Christine, Yun, Sujin, White, Allison, Nguyen, Leslie, Koudriakova, Tatiana, Tian, Gaochao, Suarez, Javier, Szewczuk, Lawrence, Bonnette, William, Ahn, Kay, Ghosh, Brahma, Flores, Christopher M, Connolly, Peter J, Zhu, Bin, Macielag, Mark J, Brandt, Michael R, Chevalier, Kristen, Zhang, Sui-Po, Lovenberg, Timothy, Bonaventure, Pascal

“…The serine hydrolase monoacylglycerol lipase (MAGL) is the rate-limiting enzyme responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol…”
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In Vitro Antibacterial Activities of JNJ-Q2, a New Broad-Spectrum Fluoroquinolone by MORROW, Brian J, WENPING HE, AMSLER, Karen M, FOLENO, Barbara D, MACIELAG, Mark J, LYNCH, A. Simon, BUSHT, Karen

“…OA  Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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GPR120 agonists for the treatment of diabetes: a patent review (2014 present) by Zhang, Xuqing, Macielag, Mark J

“…G protein-coupled receptor 120 (GPR120) is a G coupled GPCR specifically activated by long-chain fatty acids (LCFAs). Functionally, it has been identified as a…”
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In Vivo Activity of the Pyrrolopyrazolyl-Substituted Oxazolidinone RWJ-416457 by HILLIARD, Jamese J, FERNANDEZ, Jeffrey, MELTON, John, MACIELAG, Mark J, GOLDSCHMIDT, Raul, BUSH, Karen, ABBANAT, Darren

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New β-lactam antibiotics and β-lactamase inhibitors by Bush, Karen, Macielag, Mark J

“…β-Lactam antibiotics are among the most frequently prescribed antibiotics used to treat bacterial infections. However, their utility is being threatened by the…”
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Discovery of Potent and Orally Bioavailable Pyridine N‑Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions by Xu, Guozhang, Liu, Zhijie, Wang, Xinkang, Lu, Tianbao, DesJarlais, Renee L., Thieu, Tho, Zhang, Jing, Devine, Zheng Huang, Du, Fuyong, Li, Qiu, Milligan, Cynthia M., Shaffer, Paul, Cedervall, Peder E., Spurlino, John C., Stratton, Christopher F., Pietrak, Beth, Szewczuk, Lawrence M., Wong, Victoria, Steele, Ruth A., Bruinzeel, Wouter, Chintala, Madhu, Silva, Jose, Gaul, Michael D., Macielag, Mark J., Nargund, Ravi

“…Activated factor XI (FXIa) inhibitors are promising novel anticoagulants with low bleeding risk compared with current anticoagulants. The discovery of potent…”
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In Vitro Antibacterial Activity of the Pyrrolopyrazolyl-Substituted Oxazolidinone RWJ-416457 by FOLENO, Barbara D, ABBANAT, Darren, GOLDSCHMIDT, Raul M, FLAMM, Robert K, PAGET, Steve D, WEBB, Glenda C, WIRA, Ellyn, MACIELAG, Mark J, BUSH, Karen

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The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL) by Zhu, Bin, Connolly, Peter J., Zhang, Sui-Po, Chevalier, Kristen M., Milligan, Cynthia M., Flores, Christopher M., Macielag, Mark J.

“…[Display omitted] Monoacylglycerol lipase (MAGL) has emerged as an attractive drug target because of its important role in regulating the endocannabinoid…”
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Design, synthesis and preclinical evaluation of bio-conjugated amylinomimetic peptides as long-acting amylin receptor agonists by Patch, Raymond J., Zhang, Rui, Edavettal, Suzanne, Macielag, Mark J., Eckardt, Annette J., Li, Jiali, Rives, Marie-Laure, Edwards, Wilson, Hinke, Simon A., Qiu, Xi, Jian, Wenying, Libiger, Ondrej, Zheng, Songmao, Jeyaseelan, Jey, Liang, Yin, Rangwala, Shamina M., Leonard, James N., Hornby, Pamela

“…Pramlintide is an equipotent amylin analogue that reduces food intake and body weight in obese subjects and has been clinically approved as an adjunctive…”
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The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors by Zhu, Bin, Connolly, Peter J., Zhang, Yue-Mei, McDonnell, Mark E., Bian, Haiyan, Lin, Shu-Chen, Liu, Li, Zhang, Sui-Po, Chevalier, Kristen M., Brandt, Michael R., Milligan, Cynthia M., Flores, Christopher M., Macielag, Mark J.

“…[Display omitted] Monoacylglycerol lipase (MAGL) is the enzyme that is primarily responsible for hydrolyzing the endocannabinoid 2-arachidononylglycerol (2-AG)…”
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6‑Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB1) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity by Zhang, Yue-Mei, Greco, Michael N, Macielag, Mark J, Teleha, Christopher A, DesJarlais, Renee L, Tang, Yuting, Ho, George, Hou, Cuifen, Chen, Cailin, Zhao, Shuyuan, Kauffman, Jack, Camacho, Raul, Qi, Jenson, Murray, William, Demarest, Keith, Leonard, James

“…A novel series of 6-benzhydryl-4-amino-quinolin-2-ones was discovered as cannabinoid type 1 receptor (CB1R) inverse agonists based on the high-throughput…”
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Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes by Zhang, Xuqing, Zhu, Bin, Guo, Lili, Bakaj, Ivona, Rankin, Matthew, Ho, George, Kauffman, Jack, Lee, Seunghun P, Norquay, Lisa, Macielag, Mark J

“…A novel series of pyridones were discovered as potent EP3 antagonists. Optimization guided by EP3 binding and functional assays as well as by eADME and PK…”
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Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists by Matthews, Jay M., McNally, James J., Connolly, Peter J., Xia, Mingde, Zhu, Bin, Black, Shawn, Chen, Cailin, Hou, Cuifen, Liang, Yin, Tang, Yuting, Macielag, Mark J.

“…[Display omitted] A series of potent and receptor-selective cannabinoid-1 (CB1) receptor inverse agonists has been discovered. Peripheral selectivity of the…”
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Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 Å resolution by Schalk‐Hihi, Céline, Schubert, Carsten, Alexander, Richard, Bayoumy, Shariff, Clemente, Jose C., Deckman, Ingrid, DesJarlais, Renee L., Dzordzorme, Keli C., Flores, Christopher M., Grasberger, Bruce, Kranz, James K., Lewandowski, Frank, Liu, Li, Ma, Hongchang, Maguire, Diane, Macielag, Mark J., McDonnell, Mark E., Mezzasalma Haarlander, Tara, Miller, Robyn, Milligan, Cindy, Reynolds, Charles, Kuo, Lawrence C.

“…A high‐resolution structure of a ligand‐bound, soluble form of human monoglyceride lipase (MGL) is presented. The structure highlights a novel conformation of…”
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Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists by Zhu, Bin, Matthews, Jay M., Xia, Mingde, Black, Shawn, Chen, Cailin, Hou, Cuifen, Liang, Yin, Tang, Yuting, Macielag, Mark J.

“…[Display omitted] Peripherally restricted CB1 receptor inverse agonists hold potential as useful therapeutics to treat obesity and related metabolic diseases…”
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Anti-MRSA beta-lactams in development, with a focus on ceftobiprole: the first anti-MRSA beta-lactam to demonstrate clinical efficacy by Bush, Karen, Heep, Markus, Macielag, Mark J, Noel, Gary J

“…Ceftobiprole is the first of the investigational beta-lactam antibiotics with in vitro activity against methicillin-resistant staphylococci to reach and…”
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The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones by Weidner-Wells, Michele A., Werblood, Harvey M., Goldschmidt, Raul, Bush, Karen, Foleno, Barbara D., Hilliard, Jamese J., Melton, John, Wira, Ellyn, Macielag, Mark J.

“…A series of oxazolidinone antibacterial agents containing a 5-substituted isoxazol-3-yl moiety were synthesized via a nitrile oxide [3+2] dipolar cycloaddition…”
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Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists by Zhu, Bin, Xia, Mingde, Xu, Xiaoqing, Ludovici, Donald W., Tennakoon, Manomi, Youngman, Mark A., Matthews, Jay M., Dax, Scott L., Colburn, Raymond W., Qin, Ning, Hutchinson, Tasha L., Lubin, Mary Lou, Brandt, Michael R., Stone, Dennis J., Flores, Christopher M., Macielag, Mark J.

“…A series of arylglycine-based analogs was synthesized and tested for TRPM8 antagonism in a cell-based functional assay. Following structure–activity…”
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7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors by Grant, Eugene B., Foleno, Barbara D., Goldschmidt, Raul, Hilliard, Jamese J., Lin, Shu-Chen, Morrow, Brian, Paget, Steven D., Weidner-Wells, Michele A., Xu, Xiaodong, Xu, Xiaoqing, Murray, William V., Bush, Karen, Macielag, Mark J.

“…[Display omitted] Novel antibacterial fluoroquinolone agents bearing a 4-alkylidenylpiperidine 7-position substituent are active against quinolone-susceptible…”
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Synthesis and antibacterial activity of 3-keto-6- O-carbamoyl-11,12-cyclic thiocarbamate erythromycin A derivatives by Zhu, Bin, Marinelli, Brett A., Abbanat, Darren, Foleno, Barbara D., Bush, Karen, Macielag, Mark J.

“…A series of 3-keto-6- O-carbamoyl-11,12-cyclic thiocarbamate erythromycin A derivatives has been synthesized. The best compounds in this series possess potent…”
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