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21 results on '"Neckermann, Georg"'

3. Abstract 4851: Potent cell cycle inhibitors suitable for treatment of multidrug-resistant tumors

Author

Sivaraja, Mohan, primary, Sizikov, Sivan, additional, Sirisoma, Nilantha, additional, Kirtadze, Tamari, additional, Chattopadhyay, Madhuri, additional, Ewald, Makena, additional, Dash, Subhadra, additional, Wong, Anne, additional, Neckermann, Georg, additional, To, Elaine, additional, Chang, Stephanie, additional, Shiau, Timothy P., additional, Williams, David C., additional, Short, Kevin M., additional, Estiarte, Angels, additional, Datta, Anirban, additional, and Kita, David B., additional

Published
2018
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4. Antibacterial and Solubility Optimization of Thiomuracin A

Author

LaMarche, Matthew J., primary, Leeds, Jennifer A., additional, Brewer, Jason, additional, Dean, Karl, additional, Ding, Jian, additional, Dzink-Fox, Joanne, additional, Gamber, Gabe, additional, Jain, Akash, additional, Kerrigan, Ryan, additional, Krastel, Philipp, additional, Lee, Kwangho, additional, Lombardo, Franco, additional, McKenney, David, additional, Neckermann, Georg, additional, Osborne, Colin, additional, Palestrant, Deborah, additional, Patane, Michael A., additional, Rann, Elin M., additional, Robinson, Zachary, additional, Schmitt, Esther, additional, Stams, Travis, additional, Tiamfook, Stacey, additional, Yu, Donghui, additional, and Whitehead, Lewis, additional

Published
2016
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5. SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1

Author

Huang, Wenlin, primary, Ojo, Kayode K., additional, Zhang, Zhongsheng, additional, Rivas, Kasey, additional, Vidadala, Rama Subba Rao, additional, Scheele, Suzanne, additional, DeRocher, Amy E., additional, Choi, Ryan, additional, Hulverson, Matthew A., additional, Barrett, Lynn K., additional, Bruzual, Igor, additional, Siddaramaiah, Latha Kallur, additional, Kerchner, Keshia M., additional, Kurnick, Matthew D., additional, Freiberg, Gail M., additional, Kempf, Dale, additional, Hol, Wim G. J., additional, Merritt, Ethan A., additional, Neckermann, Georg, additional, de Hostos, Eugenio L., additional, Isoherranen, Nina, additional, Maly, Dustin J., additional, Parsons, Marilyn, additional, Doggett, J. Stone, additional, Van Voorhis, Wesley C., additional, and Fan, Erkang, additional

Published
2015
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6. Mo1233 Pharmacologic Evaluation of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea

Author

Griggs, David W., primary, Prinsen, Michael J., additional, Campbell, Mary, additional, Oliva, Jonathan, additional, Ruminski, Peter, additional, Yu, Ying, additional, Bond, Brian R., additional, Ji, Yuhua, additional, Neckermann, Georg, additional, Choy, Robert, additional, de Hostos, Eugenio L., additional, and Meyers, Marvin, additional

Published
2015
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7. Discovery of Inhibitors of 4′-Phosphopantetheine Adenylyltransferase (PPAT) To Validate PPAT as a Target for Antibacterial Therapy

Author

de Jonge, Boudewijn L. M., primary, Walkup, Grant K., additional, Lahiri, Sushmita D., additional, Huynh, Hoan, additional, Neckermann, Georg, additional, Utley, Luke, additional, Nash, Tory J., additional, Brock, Jesse, additional, San Martin, Maryann, additional, Kutschke, Amy, additional, Johnstone, Michele, additional, Laganas, Valerie, additional, Hajec, Laurel, additional, Gu, Rong-Fang, additional, Ni, Haihong, additional, Chen, Brendan, additional, Hutchings, Kim, additional, Holt, Elise, additional, McKinney, David, additional, Gao, Ning, additional, Livchak, Stephania, additional, and Thresher, Jason, additional

Published
2013
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10. Antibacterial Optimization of 4-Aminothiazolyl Analogues of the Natural Product GE2270 A: Identification of the Cycloalkylcarboxylic Acids

Author

LaMarche, Matthew J., primary, Leeds, Jennifer A., additional, Amaral, Kerri, additional, Brewer, Jason T., additional, Bushell, Simon M., additional, Dewhurst, Janetta M., additional, Dzink-Fox, JoAnne, additional, Gangl, Eric, additional, Goldovitz, Julie, additional, Jain, Akash, additional, Mullin, Steve, additional, Neckermann, Georg, additional, Osborne, Colin, additional, Palestrant, Deborah, additional, Patane, Michael A., additional, Rann, Elin M., additional, Sachdeva, Meena, additional, Shao, Jian, additional, Tiamfook, Stacey, additional, Whitehead, Lewis, additional, and Yu, Donghui, additional

Published
2011
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13. Hepatobiliary transport of hepatic 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitors conjugated with bile acids

Author

Petzinger, Ernst, primary, Nickau, Lutz, additional, Horz, Jurgen A., additional, Schulz, Siegfried, additional, Wess, Gunther, additional, Enhsen, Alfons, additional, Falk, Eugen, additional, Baringhaus, Karl-Heinz, additional, Glombik, Heiner, additional, Hoffmann, Axel, additional, Müllner, Stefan, additional, Neckermann, Georg, additional, and Kramer, Werner, additional

Published
1995
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20. Bile acid derived HMG-CoA reductase inhibitors

Author

Kramer, Werner, Wess, Günther, Enhsen, Alfons, Bock, Klaus, Falk, Eugen, Hoffman, Axel, Neckermann, Georg, Gantz, Dietrich, Schulz, Siefried, Nickau, Lutz, Petzinger, Ernst, Turley, Stephen, and Dietschy, John M.

Published
1994
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21. Pharmacologic Comparison of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea.

Author

Griggs DW, Prinsen MJ, Oliva J, Campbell MA, Arnett SD, Tajfirouz D, Ruminski PG, Yu Y, Bond BR, Ji Y, Neckermann G, Choy RK, de Hostos E, and Meyers MJ

Subjects
Animals, Castor Oil, Charcoal pharmacology, Diarrhea chemically induced, Dose-Response Relationship, Drug, Feces, Gastrointestinal Motility drug effects, Male, Rats, Rats, Wistar, Thiorphan therapeutic use, Antidiarrheals therapeutic use, Diarrhea drug therapy, Endopeptidases metabolism, Protease Inhibitors therapeutic use, Thiorphan analogs & derivatives
Abstract

Racecadotril (acetorphan) is a neutral endopeptidase (NEP) inhibitor with known antidiarrheal activity in animals and humans; however, in humans, it suffers from shortcomings that might be improved with newer drugs in this class that have progressed to the clinic for nonenteric disease indications. To identify potentially superior NEP inhibitors with immediate clinical utility for diarrhea treatment, we compared their efficacy and pharmacologic properties in a rat intestinal hypersecretion model. Racecadotril and seven other clinical-stage inhibitors of NEP were obtained or synthesized. Enzyme potency and specificity were compared using purified peptidases. Compounds were orally administered to rats before administration of castor oil to induce diarrhea. Stool weight was recorded over 4 hours. To assess other pharmacologic properties, select compounds were orally administered to normal or castor oil-treated rats, blood and tissue samples collected at multiple time points, and active compound concentrations determined by mass spectroscopy. NEP enzyme activity was measured in tissue homogenates. Three previously untested clinical NEP inhibitors delayed diarrhea onset and reduced total stool output, with little or no effect on intestinal motility assessed by the charcoal meal test. Each was shown to be a potent, highly specific inhibitor of NEP. Each exhibited greater suppression of NEP activity in intestinal and nonintestinal tissues than did racecadotril and sustained this inhibition longer. These results suggest that newer clinical-stage NEP inhibitors originally developed for other indications may be directly repositioned for treatment of acute secretory diarrhea and offer advantages over racecadotril, such as less frequent dosing and potentially improved efficacy., (Copyright © 2016 The Author(s).)

Published
2016
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