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1. Towards the sustainable discovery and development of new antibiotics

Author

Miethke, Marcus, Pieroni, Marco, Weber, Tilmann, Brönstrup, Mark, Hammann, Peter, Halby, Ludovic, Arimondo, Paola B., Glaser, Philippe, Aigle, Bertrand, Bode, Helge B., Moreira, Rui, Li, Yanyan, Luzhetskyy, Andriy, Medema, Marnix H., Pernodet, Jean-Luc, Stadler, Marc, Tormo, José Rubén, Genilloud, Olga, Truman, Andrew W., Weissman, Kira J., Takano, Eriko, Sabatini, Stefano, Stegmann, Evi, Brötz-Oesterhelt, Heike, Wohlleben, Wolfgang, Seemann, Myriam, Empting, Martin, Hirsch, Anna K. H., Loretz, Brigitta, Lehr, Claus-Michael, Titz, Alexander, Herrmann, Jennifer, Jaeger, Timo, Alt, Silke, Hesterkamp, Thomas, Winterhalter, Mathias, Schiefer, Andrea, Pfarr, Kenneth, Hoerauf, Achim, Graz, Heather, Graz, Michael, Lindvall, Mika, Ramurthy, Savithri, Karlén, Anders, van Dongen, Maarten, Petkovic, Hrvoje, Keller, Andreas, Peyrane, Frédéric, Donadio, Stefano, Fraisse, Laurent, Piddock, Laura J. V., Gilbert, Ian H., Moser, Heinz E., and Müller, Rolf

Published
2021
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2. Aminoglycosides

Author

Armstrong, Eliana S., Kostrub, Corwin F., Cass, Robert T., Moser, Heinz E., Serio, Alisa W., Miller, George H., Dougherty, Thomas J., editor, and Pucci, Michael J., editor

Published
2012
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3. In Vitro and In Vivo Properties of CUO246, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor

Author

Blais, Johanne, primary, Dean, Charles R., additional, Lapointe, Guillaume, additional, Leeds, Jennifer A., additional, Ma, Sylvia, additional, Morris, Laura, additional, Moser, Heinz E., additional, Osborne, Colin S., additional, Prosen, Katherine R., additional, Richie, Daryl, additional, Skepper, Colin, additional, Thompson, Katherine, additional, Vo, Jason, additional, Yue, Qin, additional, and Rivkin, Alexey, additional

Published
2022
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5. Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria

Author

Lapointe, Guillaume, primary, Skepper, Colin K., additional, Holder, Lauren M., additional, Armstrong, Duncan, additional, Bellamacina, Cornelia, additional, Blais, Johanne, additional, Bussiere, Dirksen, additional, Bian, Jianwei, additional, Cepura, Cody, additional, Chan, Helen, additional, Dean, Charles R., additional, De Pascale, Gianfranco, additional, Dhumale, Bhavesh, additional, Fisher, L. Mark, additional, Fulsunder, Mangesh, additional, Kantariya, Bhavin, additional, Kim, Julie, additional, King, Sean, additional, Kossy, Lauren, additional, Kulkarni, Upendra, additional, Lakshman, Jay, additional, Leeds, Jennifer A., additional, Ling, Xiaolan, additional, Lvov, Anatoli, additional, Ma, Sylvia, additional, Malekar, Swapnil, additional, McKenney, David, additional, Mergo, Wosenu, additional, Metzger, Louis, additional, Mhaske, Keshav, additional, Moser, Heinz E., additional, Mostafavi, Mina, additional, Namballa, Sunil, additional, Noeske, Jonas, additional, Osborne, Colin, additional, Patel, Ashish, additional, Patel, Darshit, additional, Patel, Tushar, additional, Piechon, Philippe, additional, Polyakov, Valery, additional, Prajapati, Krunal, additional, Prosen, Katherine R., additional, Reck, Folkert, additional, Richie, Daryl L., additional, Sanderson, Mark R., additional, Satasia, Shailesh, additional, Savani, Bhautik, additional, Selvarajah, Jogitha, additional, Sethuraman, Vijay, additional, Shu, Wei, additional, Tashiro, Kyuto, additional, Thompson, Katherine V., additional, Vaarla, Krishniah, additional, Vala, Lakhan, additional, Veselkov, Dennis A., additional, Vo, Jason, additional, Vora, Bhavesh, additional, Wagner, Trixie, additional, Wedel, Laura, additional, Williams, Sarah L., additional, Yendluri, Satya, additional, Yue, Qin, additional, Yifru, Aregahegn, additional, Zhang, Yong, additional, and Rivkin, Alexey, additional

Published
2021
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6. Aminoglycosides

Author

Armstrong, Eliana S., primary, Kostrub, Corwin F., additional, Cass, Robert T., additional, Moser, Heinz E., additional, Serio, Alisa W., additional, and Miller, George H., additional

Published
2011
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8. Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria

Author

Skepper, Colin K., primary, Armstrong, Duncan, additional, Balibar, Carl J., additional, Bauer, Daniel, additional, Bellamacina, Cornelia, additional, Benton, Bret M., additional, Bussiere, Dirksen, additional, De Pascale, Gianfranco, additional, De Vicente, Javier, additional, Dean, Charles R., additional, Dhumale, Bhavesh, additional, Fisher, L. Mark, additional, Fuller, John, additional, Fulsunder, Mangesh, additional, Holder, Lauren M., additional, Hu, Cheng, additional, Kantariya, Bhavin, additional, Lapointe, Guillaume, additional, Leeds, Jennifer A., additional, Li, Xiaolin, additional, Lu, Peichao, additional, Lvov, Anatoli, additional, Ma, Sylvia, additional, Madhavan, Shravanthi, additional, Malekar, Swapnil, additional, McKenney, David, additional, Mergo, Wosenu, additional, Metzger, Louis, additional, Moser, Heinz E., additional, Mutnick, Daniel, additional, Noeske, Jonas, additional, Osborne, Colin, additional, Patel, Ashish, additional, Patel, Darshit, additional, Patel, Tushar, additional, Prajapati, Krunal, additional, Prosen, Katherine R., additional, Reck, Folkert, additional, Richie, Daryl L., additional, Rico, Alice, additional, Sanderson, Mark R., additional, Satasia, Shailesh, additional, Sawyer, William S., additional, Selvarajah, Jogitha, additional, Shah, Nirav, additional, Shanghavi, Kartik, additional, Shu, Wei, additional, Thompson, Katherine V., additional, Traebert, Martin, additional, Vala, Anand, additional, Vala, Lakhan, additional, Veselkov, Dennis A., additional, Vo, Jason, additional, Wang, Michael, additional, Widya, Marcella, additional, Williams, Sarah L., additional, Xu, Yongjin, additional, Yue, Qin, additional, Zang, Richard, additional, Zhou, Bo, additional, and Rivkin, Alexey, additional

Published
2020
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9. Creating RNA bulges: cleavage of RNA in RNA/DNA duplexes by metal ion catalysis

Author

Husken, Dieter, Goodall, Greg, Blommers, Marcel J.J., Jahnke, Wolfgang, Hall, Jonathan, Haner, Robert, and Moser, Heinz E.

Subjects
RNA -- Research, DNA -- Research, Nucleotides -- Research, Biological sciences, Chemistry
Abstract

A single-stranded RNA target was manipulated to produce various RNA/antisense hybrids illustrating the possibility of cleaving the RNA strand within duplexes. This was accomplished by sequence composition of the antisense oligonucleotide, a technique which produced various bulges in the RNA target, which is then cleavable at these specific bulge sites under free meal ion or metal complex catalysis.

Published
1996

10. Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae – Identification of LYS228

Author

Reck, Folkert, Bermingham, Alun, Blais, Johanne, Capka, Vladimir, Cariaga, Taryn, Casarez, Anthony, Colvin, Richard, Dean, Charles R., Fekete, Alex, Gong, Wanben, Growcott, Ellie, Guo, Hongqiu, Jones, Adriana K., Li, Cindy, Li, Fengxia, Lin, Xiaodong, Lindvall, Mika, Lopez, Sara, McKenney, David, Metzger, Louis, Moser, Heinz E., Prathapam, Ramadevi, Rasper, Dita, Rudewicz, Patrick, Sethuraman, Vijay, Shen, Xiaoyu, Shaul, Jacob, Simmons, Robert L., Tashiro, Kyuto, Tang, Dazhi, Tjandra, Meiliana, Turner, Nancy, Uehara, Tsuyoshi, Vitt, Charles, Whitebread, Steven, Yifru, Aregahegn, Zang, Xu, and Zhu, Qingming

Published
2018
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13. Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety

Author

Cohen, Frederick, primary, Aggen, James B., additional, Andrews, Logan D., additional, Assar, Zahra, additional, Boggs, Jen, additional, Choi, Taylor, additional, Dozzo, Paola, additional, Easterday, Ashton N., additional, Haglund, Cat M., additional, Hildebrandt, Darin J., additional, Holt, Melissa C., additional, Joly, Kristin, additional, Jubb, Adrian, additional, Kamal, Zeeshan, additional, Kane, Timothy R., additional, Konradi, Andrei W., additional, Krause, Kevin M., additional, Linsell, Martin S., additional, Machajewski, Timothy D., additional, Miroshnikova, Olga, additional, Moser, Heinz E., additional, Nieto, Vincent, additional, Phan, Thu, additional, Plato, Craig, additional, Serio, Alisa W., additional, Seroogy, Julie, additional, Shakhmin, Anton, additional, Stein, Adam J., additional, Sun, Alex D., additional, Sviridov, Serguei, additional, Wang, Zhan, additional, Wlasichuk, Kenneth, additional, Yang, Wen, additional, Zhou, Xiaoming, additional, Zhu, Hai, additional, and Cirz, Ryan T., additional

Published
2019
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16. Exploring the active site of the Streptococcus pneumoniae topoisomerase IV–DNA cleavage complex with novel 7,8-bridged fluoroquinolones

Author

Laponogov, Ivan, Pan, Xiao-Su, Veselkov, Dennis A., Cirz, Ryan T., Wagman, Allan, Moser, Heinz E., Fisher, L. Mark, and Sanderson, Mark R.

Subjects
drug design, Research, Topoisomerases, Protein-DNA complexes, protein–DNA complexes, Drug design, topoisomerases, MIC determinants, DNA topological experiments, lcsh:Biology (General), lcsh:QH301-705.5, Research Article, X-ray crystallography
Abstract

As part of a programme of synthesizing and investigating the biological properties of new fluoroquinolone antibacterials and their targeting of topoisomerase IV from Streptococcus pneumoniae, we have solved the X-ray structure of the complexes of two new 7,8-bridged fluoroquinolones (with restricted C7 group rotation favouring tight binding) in complex with the topoisomerase IV from S. pneumoniae and an 18-base-pair DNA binding site-the E-site-found by our DNA mapping studies to bind drug strongly in the presence of topoisomerase IV (Leo et al. 2005 J. Biol. Chem. 280, 14 252-14 263, doi:10.1074/jbc.M500156200). Although the degree of antibiotic resistance towards fluoroquinolones is much lower than that of β-lactams and a range of ribosome-bound antibiotics, there is a pressing need to increase the diversity of members of this successful clinically used class of drugs. The quinolone moiety of the new 7,8-bridged agents ACHN-245 and ACHN-454 binds similarly to that of clinafloxocin, levofloxacin, moxifloxacin and trovofloxacin but the cyclic scaffold offers the possibility of chemical modification to produce interactions with other topoisomerase residues at the active site.

Published
2016
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17. Studies of prokaryotic Type II topoisomerase drug inhibition

Author

Sanderson, Mark R., primary, Laponogov, Ivan, additional, Pan, Xiaosu, additional, Veselkov, Dennis A., additional, Crevel, Isabelle M.-T., additional, Selvarajah, Jogitha, additional, Branstrom, Art, additional, Cirz, Ryan, additional, Moser, Heinz E., additional, and Fisher, L. Mark, additional

Published
2017
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18. Cover Feature: Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones (ChemMedChem 20/2017)

Author

Wagman, Allan S., primary, Cirz, Ryan, additional, McEnroe, Glenn, additional, Aggen, James, additional, Linsell, Martin S., additional, Goldblum, Adam A., additional, Lopez, Sara, additional, Gomez, Marcela, additional, Miller, George, additional, Simons, Lloyd J., additional, Belliotti, Thomas R., additional, Harris, Christina R., additional, Poel, Toni-Jo, additional, Melnick, Michael J., additional, Gaston, Ricky D., additional, and Moser, Heinz E., additional

Published
2017
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19. Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones

Author

Wagman, Allan S., primary, Cirz, Ryan, additional, McEnroe, Glenn, additional, Aggen, James, additional, Linsell, Martin S., additional, Goldblum, Adam A., additional, Lopez, Sara, additional, Gomez, Marcela, additional, Miller, George, additional, Simons, Lloyd J., additional, Belliotti, Thomas R., additional, Harris, Christina R., additional, Poel, Toni‐Jo, additional, Melnick, Michael J., additional, Gaston, Ricky D., additional, and Moser, Heinz E., additional

Published
2017
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21. Synthesis and Spectrum of the Neoglycoside ACHN-490

Author

Aggen, James B., primary, Armstrong, Eliana S., additional, Goldblum, Adam A., additional, Dozzo, Paola, additional, Linsell, Martin S., additional, Gliedt, Micah J., additional, Hildebrandt, Darin J., additional, Feeney, Lee Ann, additional, Kubo, Aya, additional, Matias, Rowena D., additional, Lopez, Sara, additional, Gomez, Marcela, additional, Wlasichuk, Kenneth B., additional, Diokno, Raymond, additional, Miller, George H., additional, and Moser, Heinz E., additional

Published
2010
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23. Potent and selective xanthine-based inhibitors of phosphodiesterase 5

Author

Arnold, Nichola J., Arnold, Ruth, Beer, David, Bhalay, Gurdip, Collingwood, Stephen P., Craig, Sarah, Devereux, Nicholas, Dodds, Mark, Dunstan, Andrew R., Fairhurst, Robin A., Farr, David, Fullerton, Joseph D., Glen, Angela, Gomez, Sylvie, Haberthuer, Sandra, Hatto, Julia D.I., Howes, Colin, Jones, Darryl, Keller, Thomas H., Leuenberger, Beate, Moser, Heinz E., Muller, Irene, Naef, Reto, Nicklin, Paul A., Sandham, David A., Turner, Katharine L., Tweed, Morris F., Watson, Simon J., and Zurini, Mauro

Published
2007
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28. DNA Binding Ligands with Improved in Vitro and in Vivo Potency against Drug-Resistant Staphylococcus aureus

Author

Hu, Wenhao, primary, Bürli, Roland W., additional, Kaizerman, Jacob A., additional, Johnson, Kirk W., additional, Gross, Matthew I., additional, Iwamoto, Mari, additional, Jones, Peter, additional, Lofland, Denene, additional, Difuntorum, Stacey, additional, Chen, Hsiu, additional, Bozdogan, Bülent, additional, Appelbaum, Peter C., additional, and Moser, Heinz E., additional

Published
2004
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31. DNA binding ligands with in vivo efficacy in murine models of bacterial infection: optimization of internal aromatic amino acids

Author

Bürli, Roland W., primary, Kaizerman, Jacob A., additional, Duan, Jian-Xin, additional, Jones, Peter, additional, Johnson, Kirk W., additional, Iwamoto, Mari, additional, Truong, Kiet, additional, Hu, Wenhao, additional, Stanton, Timothy, additional, Chen, Alfred, additional, Touami, Sofia, additional, Gross, Matthew, additional, Jiang, Vernon, additional, Ge, Yigong, additional, and Moser, Heinz E., additional

Published
2004
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40. Second Generation of Antisense Oligonucleotides: From Nuclease Resistance to Biological Efficacy in Animals

Author

Altmann, Karl-Heinz, primary, Dean, Nicholas M., additional, Fabbro, Doriano, additional, Freier, Susan M., additional, Geiger, Thomas, additional, Häner, Robert, additional, Hüsken, Dieter, additional, Martin, Pierre, additional, Monia, Brett P., additional, Müller, Marcel, additional, Natt, François, additional, Nicklin, Paul, additional, Phillips, Judy, additional, Pieles, Uwe, additional, Sasmor, Henri, additional, and Moser, Heinz E., additional

Published
1996
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49. Macrocyclic inhibitors for peptide deformylase: a structure-activity relationship study of the ring size.

Author

Hu X, Nguyen KT, Jiang VC, Lofland D, Moser HE, and Pei D

Subjects
Amidohydrolases chemistry, Amidohydrolases metabolism, Animals, Binding Sites, Drug Evaluation, Preclinical methods, Drug Stability, Humans, Microbial Sensitivity Tests, Rats, Structure-Activity Relationship, Amidohydrolases antagonists & inhibitors, Anti-Bacterial Agents chemistry, Anti-Bacterial Agents pharmacology, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Heterocyclic Compounds chemistry
Abstract

Peptide deformylase (PDF) catalyzes the removal of the N-terminal formyl group from newly synthesized polypeptides in eubacteria. Its essential role in bacterial cells but not in mammalian cells makes it an attractive target for antibacterial drug design. We have previously reported an N-formylhydroxylamine-based, metal-chelating macrocyclic PDF inhibitor, in which the P(1)' and P(3)' side chains are covalently joined. In this work, we have carried out a structure-activity relationship study on the size of the macrocycle and found that 15-17-membered macrocycles are optimal for binding to the PDF active site. Unlike the acyclic compounds, which are simple competitive inhibitors, the cyclic compounds all act as slow-binding inhibitors. As compared to their acyclic counterparts, the cyclic inhibitors displayed 20-50-fold higher potency against the PDF active site (K(I) as low as 70 pM), improved selectivity toward PDF, and improved the metabolic stability in rat plasma. Some of the macrocyclic inhibitors had potent, broad spectrum antibacterial activity against clinically significant Gram-positive and Gram-negative pathogens. These results suggest that the macrocyclic scaffold provides an excellent lead for the development of a new class of antibiotics.

Published
2004
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50. Dual Recognition of Double-Stranded DNA by 2'-Aminoethoxy-Modified Oligonucleotides.

Author

Cuenoud B, Casset F, Hüsken D, Natt F, Wolf RM, Altmann KH, Martin P, and Moser HE

Abstract

Simultaneous interaction of the 2'-aminoethoxy-modified oligonucleotides with the phosphodiester backbone (shown on the right, A) and with the bases through Hoogsteen base contacts (B) is seen at each base-pair step of the duplex DNA target. The electrostatic interaction between the protonated amino group and the negatively charged phosphate group provides for a dramatic increase in the binding affinity and the association rate constant., (© 1998 WILEY-VCH Verlag GmbH, Weinheim, Fed. Rep. of Germany.)

Published
1998
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