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Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity.
Green SR, Wilson C, Eadsforth TC, Punekar AS, Tamaki FK, Wood G, Caldwell N, Forte B, Norcross NR, Kiczun M, Post JM, Lopez-Román EM, Engelhart CA, Lukac I, Zuccotto F, Epemolu O, Boshoff HIM, Schnappinger D, Walpole C, Gilbert IH, Read KD, Wyatt PG, Baragaña B. Green SR, et al. Among authors: boshoff him. J Med Chem. 2023 Nov 23;66(22):15380-15408. doi: 10.1021/acs.jmedchem.3c01514. Epub 2023 Nov 10. J Med Chem. 2023. PMID: 37948640 Free PMC article.
Structure-activity relationships at the 5-position of thiolactomycin: an intact (5R)-isoprene unit is required for activity against the condensing enzymes from Mycobacterium tuberculosis and Escherichia coli.
Kim P, Zhang YM, Shenoy G, Nguyen QA, Boshoff HI, Manjunatha UH, Goodwin MB, Lonsdale J, Price AC, Miller DJ, Duncan K, White SW, Rock CO, Barry CE 3rd, Dowd CS. Kim P, et al. J Med Chem. 2006 Jan 12;49(1):159-71. doi: 10.1021/jm050825p. J Med Chem. 2006. PMID: 16392800 Free PMC article.
151 results