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Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
Lapointe, Guillaume; Skepper, Colin K; Holder, Lauren M; Armstrong, Duncan; Bellamacina, Cornelia; Blais, Johanne; Bussiere, Dirksen; Bian, Jianwei; Cepura, Cody; Chan, Helen; Dean, Charles R; De Pascale, Gianfranco; Dhumale, Bhavesh; Fisher, L Mark; Fulsunder, Mangesh; Kantariya, Bhavin; Kim, Julie; King, Sean; Kossy, Lauren; Kulkarni, Upendra; Lakshman, Jay; Leeds, Jennifer A; Ling, Xiaolan; Lvov, Anatoli; Ma, Sylvia; Malekar, Swapnil; McKenney, David; Mergo, Wosenu; Metzger, Louis; Mhaske, Keshav; Moser, Heinz E; Mostafavi, Mina; Namballa, Sunil; Noeske, Jonas; Osborne, Colin; Patel, Ashish; Patel, Darshit; Patel, Tushar; Piechon, Philippe; Polyakov, Valery; Prajapati, Krunal; Prosen, Katherine R; Reck, Folkert; Richie, Daryl L; Sanderson, Mark R; Satasia, Shailesh; Savani, Bhautik; Selvarajah, Jogitha; Sethuraman, Vijay; Shu, Wei.
Affiliation
  • Lapointe G; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Skepper CK; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Holder LM; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Armstrong D; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Bellamacina C; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Blais J; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Bussiere D; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Bian J; Novartis Global Drug Development, Pudong, Shanghai 201203, China.
  • Cepura C; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Chan H; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Dean CR; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • De Pascale G; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Dhumale B; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Fisher LM; Molecular and Clinical Sciences Research Institute, St George's, University of London, London SW17 0RE, U.K.
  • Fulsunder M; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Kantariya B; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Kim J; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • King S; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Kossy L; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Kulkarni U; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Lakshman J; Novartis Global Drug Development, East Hanover, New Jersey 07936, United States.
  • Leeds JA; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Ling X; Novartis Global Drug Development, Pudong, Shanghai 201203, China.
  • Lvov A; Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
  • Ma S; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Malekar S; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • McKenney D; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Mergo W; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Metzger L; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Mhaske K; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Moser HE; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Mostafavi M; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Namballa S; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Noeske J; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Osborne C; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Patel A; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Patel D; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Patel T; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Piechon P; Novartis Institutes for BioMedical Research, Basel 4002, Switzerland.
  • Polyakov V; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Prajapati K; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Prosen KR; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Reck F; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Richie DL; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Sanderson MR; Randall Centre for Cell and Molecular Biophysics, King's College, Guy's Campus, London Bridge, London SE1 1UL, U.K.
  • Satasia S; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Savani B; Piramal Discovery Solutions, Pharmaceutical Special Economic Zone, Sarkhej Bavla Highway, Ahmedabad, Gujarat 382213, India.
  • Selvarajah J; Molecular and Clinical Sciences Research Institute, St George's, University of London, London SW17 0RE, U.K.
  • Sethuraman V; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
  • Shu W; Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
J Med Chem ; 64(9): 6329-6357, 2021 05 13.
Article in En | MEDLINE | ID: mdl-33929852
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Staphylococcus aureus / Drug Design / Fluoroquinolones / DNA Gyrase / DNA Topoisomerase IV / Topoisomerase II Inhibitors / Anti-Bacterial Agents Limits: Animals Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Type: Article Affiliation country: United States
Fulltext
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PubMed Links
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Staphylococcus aureus / Drug Design / Fluoroquinolones / DNA Gyrase / DNA Topoisomerase IV / Topoisomerase II Inhibitors / Anti-Bacterial Agents Limits: Animals Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Type: Article Affiliation country: United States