Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Aregahegn Yifru"'
Autor:
David McKenney, Louis E. Metzger, Dirksen E. Bussiere, Sylvia Ma, Ashish Patel, Bhavesh Dhumale, Upendra Kulkarni, Jay Parthiban Lakshman, Sean King, Duncan Armstrong, Kyuto Tashiro, Lauren Kossy, Tushar Patel, Lauren M. Holder, Jogitha Selvarajah, Sarah Williams, Satya Yendluri, Colin Osborne, Jason Vo, Mangesh Fulsunder, Xiaolan Ling, Laura Wedel, Gianfranco De Pascale, Jennifer A. Leeds, Cody Cepura, Heinz E. Moser, Alexey Rivkin, Sunil Namballa, Colin K. Skepper, Bhavin Kantariya, Mina Mostafavi, Bhautik Savani, Anatoli Lvov, Guillaume Lapointe, Cornelia Bellamacina, Bhavesh Vora, Daryl L. Richie, Helen Chan, Wosenu Mergo, Jianwei Bian, Wei Shu, Keshav Mhaske, Aregahegn Yifru, Mark R. Sanderson, Swapnil Malekar, Johanne Blais, Qin Yue, Yong Zhang, Katherine V. Thompson, Julie Kim, Charles R. Dean, Vijay Sethuraman, Trixie Wagner, L. Mark Fisher, Dennis A. Veselkov, Darshit Patel, Folkert Reck, Jonas Noeske, Krishniah Vaarla, Lakhan Vala, Shailesh Satasia, Krunal Prajapati, Philippe Piechon, Valery Polyakov, Katherine R Prosen
Publikováno v:
Lapointe, G, Skepper, C K, Holder, L M, Armstrong, D, Bellamacina, C, Blais, J, Bussiere, D, Bian, J, Cepura, C, Chan, H, Dean, C R, De Pascale, G, Dhumale, B, Fisher, L M, Fulsunder, M, Kantariya, B, Kim, J, King, S, Kossy, L, Kulkarni, U, Lakshman, J, Leeds, J A, Ling, X, Lvov, A, Ma, S, Malekar, S, McKenney, D, Mergo, W, Metzger, L, Mhaske, K, Moser, H E, Mostafavi, M, Namballa, S, Noeske, J, Osborne, C, Patel, A, Patel, D, Patel, T, Piechon, P, Polyakov, V, Prajapati, K, Prosen, K R, Reck, F, Richie, D L, Sanderson, M R, Satasia, S, Savani, B, Selvarajah, J, Sethuraman, V, Shu, W, Tashiro, K, Thompson, K V, Vaarla, K, Vala, L, Veselkov, D A, Vo, J, Vora, B, Wagner, T, Wedel, L, Williams, S L, Yendluri, S, Yue, Q, Yifru, A, Zhang, Y & Rivkin, A 2021, ' Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria ', Journal of Medicinal Chemistry, vol. 64, no. 9, pp. 6329-6357 . https://doi.org/10.1021/acs.jmedchem.1c00375
Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV via binding to, and stabilization of, DNA cleavage complexes. Optimization of this series led to the identification of compou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56db96726415696056387173baa99222
https://kclpure.kcl.ac.uk/en/publications/675d57ab-71d9-4244-886c-019cc57306cd
https://kclpure.kcl.ac.uk/en/publications/675d57ab-71d9-4244-886c-019cc57306cd
Autor:
Cindy Li, Xu Zang, Vijay Sethuraman, Xiaoyu Shen, Johanne Blais, Heinz E. Moser, Kyuto Tashiro, Ellie Growcott, Ramadevi Prathapam, Anthony Casarez, Aregahegn Yifru, Charles Vitt, David McKenney, Tsuyoshi Uehara, Patrick J Rudewicz, Fengxia Li, Hongqiu Guo, Adriana K. Jones, Louis E. Metzger, Wanben Gong, Jacob Shaul, Alun Bermingham, Taryn Cariaga, Richard Colvin, Xiaodong Lin, Dita M. Rasper, Mika Lindvall, Dazhi Tang, Vladimir Capka, Steven Whitebread, Sara Lopez, Meiliana Tjandra, Qingming Zhu, Nancy Turner, Robert Lowell Simmons, Charles R. Dean, Alex Fekete, Folkert Reck
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:748-755
Metallo-β-lactamases (MBLs), such as New Delhi metallo-β-lactamase (NDM-1) have spread world-wide and present a serious threat. Expression of MBLs confers resistance in Gram-negative bacteria to all classes of β-lactam antibiotics, with the except
Autor:
Patrick S. Lee, Guillaume Lapointe, Ann Marie Madera, Robert L. Simmons, Wenjian Xu, Aregahegn Yifru, Meiliana Tjandra, Subramanian Karur, Alice Rico, Katherine Thompson, Jade Bojkovic, Lili Xie, Kyoko Uehara, Amy Liu, Wei Shu, Cornelia Bellamacina, David McKenney, Laura Morris, George R. Tonn, Colin Osborne, Bret M. Benton, Laura McDowell, Jiping Fu, Zachary K. Sweeney
Publikováno v:
Journal of medicinal chemistry. 61(20)
This report summarizes the identification and synthesis of novel LpxC inhibitors aided by computational methods that leveraged numerous crystal structures. This effort led to the identification of oxazolidinone and isoxazoline inhibitors with potent
Autor:
Feng Sun, David Thomas Parker, Friedrich Schuerch, Silvio Roggo, Xiaolin Li, Zachary Kevin Sweeney, Li Cao, Nicole Meier, Bernard Riss, Christian Guenat, Wei Li, Zhaobo Gao, Jiping Fu, Jibin Zhao, Subramanian Karur, Wang Ruidong, Andrew H. Weiss, Regis Denay, Alexey Rivkin, Su Xu, Harald Schroeder, Michael Paul Capparelli, Simon Ng, Quanbing Wu, Xin Xiong, Weikuan Li, Wosenu Mergo, Christopher Becker, Robert Lowell Simmons, Amy Lu, Gai Yu, Wenjian Xu, Peichao Lu, Nicolas Wenger, Christian Zürcher, Thomas Lochmann, Meiliana Tjandra, Alexandre Luneau, Hongyong Kim, Aregahegn Yifru, Yunshan Peng, Fabrice Gallou, Jianguang Zhou, Roger Aki Fujimoto, Michael Wang
Publikováno v:
Bioorganicmedicinal chemistry. 26(4)
Synthetic modification of cyclosporin A at P3-P4 positions led to the discovery of NIM258, a next generation cyclophilin inhibitor with excellent anti-hepatitis C virus potency, with decreased transporter inhibition, and pharmacokinetics suitable for
Autor:
Brigitte Wiedmann, Michael Wang, Andrew H. Weiss, Silvio Roggo, David Thomas Parker, Robert Elling, Jiping Fu, Zachary Kevin Sweeney, Markus Furegati, Kwan Leung, Robert Lowell Simmons, Aregahegn Yifru, Subramanian Karur, Yunshan Peng, Shengtian Yang, Roger Aki Fujimoto, Lili Xie, Alexey Rivkin, Michael Paul Capparelli, Linda Xiao, Imad Hanna, Charlotte Miault, Simon Ng, Christopher Becker, Wosenu Mergo, Theresa Kasprzyk, Dallas Bednarczyk, Peichao Lu, Mark Knapp, Meiliana Tjandra, Bo Zhou, Xiaolin Li, Wenjian Xu
Publikováno v:
Journal of medicinal chemistry. 57(20)
Nonimmunosuppressive cyclophilin inhibitors have demonstrated efficacy for the treatment of hepatitis C infection (HCV). However, alisporivir, cyclosporin A, and most other cyclosporins are potent inhibitors of OATP1B1, MRP2, MDR1, and other importan
Autor:
Qingming Zhu, Bushell Simon, Stacey Tiamfook, JoAnne Dzink-Fox, Michael A. Patane, Jason T. Brewer, Deborah Palestrant, Elin M. Rann, Matthew J. LaMarche, Meena Sachdeva, Anna Trzasko, Lewis Whitehead, Jennifer A. Leeds, Steve Mullin, Janetta Dewhurst, Lac Lee, Wanlin Yan, David McKenney, Gabriel G. Gamber, Jian Ding, Aregahegn Yifru, Adam Amaral, Jian Shao, Donghui Yu, Gejing Deng, Kwangho Lee, Troy Lister, Colin P. Osborne, Akash Jain
Publikováno v:
Journal of medicinal chemistry. 55(5)
Clostridium difficile (C. difficile) is a Gram positive, anaerobic bacterium that infects the lumen of the large intestine and produces toxins. This results in a range of syndromes from mild diarrhea to severe toxic megacolon and death. Alarmingly, t