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Wilson C, Ray P, Zuccotto F, et al. Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target. J Med Chem. 2021;65(1):409-423doi: 10.1021/acs.jmedchem.1c01586.
Wilson, C., Ray, P., Zuccotto, F., Hernandez, J., Aggarwal, A., Mackenzie, C., Caldwell, N., Taylor, M., Huggett, M., Mathieson, M., Murugesan, D., Smith, A., Davis, S., Cocco, M., Parai, M. K., Acharya, A., Tamaki, F., Scullion, P., Epemolu, O., Riley, J., Stojanovski, L., Lopez-Román, E. M., Torres-Gómez, P. A., Toledo, A. M., Guijarro-Lopez, L., Camino, I., Engelhart, C. A., Schnappinger, D., Massoudi, L. M., Lenaerts, A., Robertson, G. T., Walpole, C., Matthews, D., Floyd, D., Sacchettini, J. C., Read, K. D., Encinas, L., Bates, R. H., Green, S. R., & Wyatt, P. G. (2022). Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target. Journal of medicinal chemistry, 65(1), 409-423. https://doi.org/10.1021/acs.jmedchem.1c01586
Wilson, Caroline, et al. "Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target." Journal of medicinal chemistry vol. 65,1 (2022): 409-423. doi: https://doi.org/10.1021/acs.jmedchem.1c01586
Wilson C, Ray P, Zuccotto F, Hernandez J, Aggarwal A, Mackenzie C, Caldwell N, Taylor M, Huggett M, Mathieson M, Murugesan D, Smith A, Davis S, Cocco M, Parai MK, Acharya A, Tamaki F, Scullion P, Epemolu O, Riley J, Stojanovski L, Lopez-Román EM, Torres-Gómez PA, Toledo AM, Guijarro-Lopez L, Camino I, Engelhart CA, Schnappinger D, Massoudi LM, Lenaerts A, Robertson GT, Walpole C, Matthews D, Floyd D, Sacchettini JC, Read KD, Encinas L, Bates RH, Green SR, Wyatt PG. Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target. J Med Chem. 2022 Jan 13;65(1):409-423. doi: 10.1021/acs.jmedchem.1c01586. Epub 2021 Dec 15. PMID: 34910486.
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J Med Chem. 2022 Jan 13;65(1):409-423. doi: 10.1021/acs.jmedchem.1c01586. Epub 2021 Dec 15.

Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target.

Journal of medicinal chemistry

Caroline Wilson, Peter Ray, Fabio Zuccotto, Jorge Hernandez, Anup Aggarwal, Claire Mackenzie, Nicola Caldwell, Malcolm Taylor, Margaret Huggett, Michael Mathieson, Dinakaran Murugesan, Alasdair Smith, Susan Davis, Mattia Cocco, Maloy K Parai, Arjun Acharya, Fabio Tamaki, Paul Scullion, Ola Epemolu, Jennifer Riley, Laste Stojanovski, Eva Maria Lopez-Román, Pedro Alfonso Torres-Gómez, Ana Maria Toledo, Laura Guijarro-Lopez, Isabel Camino, Curtis A Engelhart, Dirk Schnappinger, Lisa M Massoudi, Anne Lenaerts, Gregory T Robertson, Chris Walpole, David Matthews, David Floyd, James C Sacchettini, Kevin D Read, Lourdes Encinas, Robert H Bates, Simon R Green, Paul G Wyatt

Affiliations

  1. Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.
  2. Department of Biochemistry and Biophysics, Texas A&M University, College Station, Texas 77843, United States.
  3. Global Health Pharma R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
  4. Department of Microbiology and Immunology, Weill Cornell Medical College, New York, New York 10065, United States.
  5. Mycobacteria Research Laboratories, Department of Microbiology, Immunology, and Pathology, Colorado State University, 200 W. Lake Street, Fort Collins, Colorado 80523-1682, United States.
  6. Structural Genomics Consortium, Research Institute of the McGill University Health Centre, 1001 Boulevard Décarie, Site Glen Block E, ES1.1614, Montréal, Québec H4A 3J1, Canada.

PMID: 34910486 DOI: 10.1021/acs.jmedchem.1c01586

Abstract

With increasing drug resistance in tuberculosis (TB) patient populations, there is an urgent need for new drugs. Ideally, new agents should work through novel targets so that they are unencumbered by preexisting clinical resistance to current treatments. Benzofuran

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