“Upcycling” known molecules and targets for drug-resistant TB

por Roubert, Christine, Fontaine, Evelyne, Upton, Anna M
Publicado 2022

TBAJ-876 Displays Bedaquiline-Like Mycobactericidal Potency without Retaining the Parental Drug’s Uncoupler Activity

por Sarathy, Jickky Palmae, Ragunathan, Priya, Cooper, Christopher B., Upton, Anna M., Grüber, Gerhard, Dick, Thomas
Publicado 2020

Comparative Efficacy of the Novel Diarylquinoline TBAJ-587 and Bedaquiline against a Resistant Rv0678 Mutant in a Mouse Model of Tuberculosis

por Xu, Jian, Converse, Paul J., Upton, Anna M., Mdluli, Khisimuzi, Fotouhi, Nader, Nuermberger, Eric L.
Publicado 2021

Comparative Efficacy of the Novel Diarylquinoline TBAJ-876 and Bedaquiline against a Resistant Rv0678 Mutant in a Mouse Model of Tuberculosis

por Almeida, Deepak, Converse, Paul J., Li, Si-Yang, Upton, Anna M., Fotouhi, Nader, Nuermberger, Eric L.
Publicado 2021

Delamanid or pretomanid? A Solomonic judgement!

por Mudde, Saskia E., Upton, Anna M., Lenaerts, Anne, Bax, Hannelore I., De Steenwinkel, Jurriaan E. M.
Publicado 2022

TBAJ-876 Retains Bedaquiline’s Activity against Subunits c and ε of Mycobacterium tuberculosis F-ATP Synthase

por Sarathy, Jickky Palmae, Ragunathan, Priya, Shin, Joon, Cooper, Christopher B., Upton, Anna M., Grüber, Gerhard, Dick, Thomas
Publicado 2019

Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876—A Less Toxic and More Potent Analogue of Bedaquiline

por Choi, Peter J., Conole, Daniel, Sutherland, Hamish S., Blaser, Adrian, Tong, Amy S.T., Cooper, Christopher B., Upton, Anna M., Palmer, Brian D., Denny, William A.
Publicado 2020

Contribution of Pretomanid to Novel Regimens Containing Bedaquiline with either Linezolid or Moxifloxacin and Pyrazinamide in Murine Models of Tuberculosis

por Xu, Jian, Li, Si-Yang, Almeida, Deepak V., Tasneen, Rokeya, Barnes-Boyle, Kala, Converse, Paul J., Upton, Anna M., Mdluli, Khisimuzi, Fotouhi, Nader, Nuermberger, Eric L.
Publicado 2019

Predictive Modeling to Study the Treatment-Shortening Potential of Novel Tuberculosis Drug Regimens, Toward Bundling of Preclinical Data

por Mudde, Saskia E, Ayoun Alsoud, Rami, van der Meijden, Aart, Upton, Anna M, Lotlikar, Manisha U, Simonsson, Ulrika S H, Bax, Hannelore I, de Steenwinkel, Jurriaan E M
Publicado 2021

Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline

por Blaser, Adrian, Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Conole, Daniel, Franzblau, Scott G., Cooper, Christopher B., Upton, Anna M., Lotlikar, Manisha, Denny, William A., Palmer, Brian D.
Publicado 2019

Arylamine N-Acetyltransferase Is Required for Synthesis of Mycolic Acids and Complex Lipids in Mycobacterium bovis BCG and Represents a Novel Drug Target

por Bhakta, Sanjib, Besra, Gurdyal S., Upton, Anna M., Parish, Tanya, Sholto-Douglas-Vernon, Carolyn, Gibson, Kevin J.C., Knutton, Stuart, Gordon, Siamon, daSilva, Rosangela P., Anderton, Matthew C., Sim, Edith
Publicado 2004

Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

por Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Conole, Daniel, Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Upton, Anna M., Lotlikar, Manisha U., Denny, William A., Palmer, Brian D.
Publicado 2018

3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel

por Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Blaser, Adrian, Conole, Daniel, Franzblau, Scott G., Lotlikar, Manisha U., Cooper, Christopher B., Upton, Anna M., Denny, William A., Palmer, Brian D.
Publicado 2019

Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis

por Lu, Guo-Liang, Tong, Amy S.T., Conole, Daniel, Sutherland, Hamish S., Choi, Peter J., Franzblau, Scott G., Upton, Anna M., Lotlikar, Manisha U., Cooper, Christopher B., Denny, William A., Palmer, Brian D.
Publicado 2020

Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis

por Sutherland, Hamish S., Lu, Guo-Liang, Tong, Amy S.T., Conole, Daniel, Franzblau, Scott G., Upton, Anna M., Lotlikar, Manisha U., Cooper, Christopher B., Palmer, Brian D., Choi, Peter J., Denny, William A.
Publicado 2022

The Novel Oxazolidinone TBI-223 Is Effective in Three Preclinical Mouse Models of Methicillin-Resistant Staphylococcus aureus Infection

por Gordon, Oren, Dikeman, Dustin A., Ortines, Roger V., Wang, Yu, Youn, Christine, Mumtaz, Mohammed, Orlando, Nicholas, Zhang, Jeffrey, Patel, Aman M., Gough, Ethan, Kaushik, Amit, Nuermberger, Eric L., Upton, Anna M., Fotouhi, Nader, Miller, Lloyd S., Archer, Nathan K.
Publicado 2022

6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis

por Tong, Amy S. T., Choi, Peter J., Blaser, Adrian, Sutherland, Hamish S., Tsang, Sophia K. Y., Guillemont, Jerome, Motte, Magali, Cooper, Christopher B., Andries, Koen, Van den Broeck, Walter, Franzblau, Scott G., Upton, Anna M., Denny, William A., Palmer, Brian D., Conole, Daniel
Publicado 2017

Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units

por Choi, Peter J., Sutherland, Hamish S., Tong, Amy S.T., Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Lotlikar, Manisha U., Upton, Anna M., Guillemont, Jerome, Motte, Magali, Queguiner, Laurence, Andries, Koen, Van den Broeck, Walter, Denny, William A., Palmer, Brian D.
Publicado 2017

Identification of 2-Aryl-Quinolone Inhibitors of Cytochrome bd and Chemical Validation of Combination Strategies for Respiratory Inhibitors against Mycobacterium tuberculosis

por Jeffreys, Laura N., Ardrey, Alison, Hafiz, Taghreed A., Dyer, Lauri-Anne, Warman, Ashley J., Mosallam, Nada, Nixon, Gemma L., Fisher, Nicholas E., Hong, W. David, Leung, Suet C., Aljayyoussi, Ghaith, Bibby, Jaclyn, Almeida, Deepak V., Converse, Paul J., Fotouhi, Nader, Berry, Neil G., Nuermberger, Eric L., Upton, Anna M., O’Neill, Paul M., Ward, Stephen A., Biagini, Giancarlo A.
Publicado 2023

Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs

por Green, Simon R., Davis, Susan H., Damerow, Sebastian, Engelhart, Curtis A., Mathieson, Michael, Baragaña, Beatriz, Robinson, David A., Tamjar, Jevgenia, Dawson, Alice, Tamaki, Fabio K., Buchanan, Kirsteen I., Post, John, Dowers, Karen, Shepherd, Sharon M., Jansen, Chimed, Zuccotto, Fabio, Gilbert, Ian H., Epemolu, Ola, Riley, Jennifer, Stojanovski, Laste, Osuna-Cabello, Maria, Pérez-Herrán, Esther, Rebollo, María José, Guijarro López, Laura, Casado Castro, Patricia, Camino, Isabel, Kim, Heather C., Bean, James M., Nahiyaan, Navid, Rhee, Kyu Y., Wang, Qinglan, Tan, Vee Y., Boshoff, Helena I. M., Converse, Paul J., Li, Si-Yang, Chang, Yong S., Fotouhi, Nader, Upton, Anna M., Nuermberger, Eric L., Schnappinger, Dirk, Read, Kevin D., Encinas, Lourdes, Bates, Robert H., Wyatt, Paul G., Cleghorn, Laura A. T.
Publicado 2022