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A dual-targeting succinate dehydrogenase and F1Fo-ATP synthase inhibitor rapidly sterilizes replicating and non-replicating Mycobacterium tuberculosis.
Adolph C, Cheung CY, McNeil MB, Jowsey WJ, Williams ZC, Hards K, Harold LK, Aboelela A, Bujaroski RS, Buckley BJ, Tyndall JDA, Li Z, Langer JD, Preiss L, Meier T, Steyn AJC, Rhee KY, Berney M, Kelso MJ, Cook GM. Adolph C, et al. Among authors: bujaroski rs. Cell Chem Biol. 2024 Apr 18;31(4):683-698.e7. doi: 10.1016/j.chembiol.2023.12.002. Epub 2023 Dec 26. Cell Chem Biol. 2024. PMID: 38151019
6-Furopyridine Hexamethylene Amiloride Is a Non-Selective P2X7 Receptor Antagonist.
Cuthbertson P, Elhage A, Al-Rifai D, Sophocleous RA, Turner RJ, Aboelela A, Majed H, Bujaroski RS, Jalilian I, Kelso MJ, Watson D, Buckley BJ, Sluyter R. Cuthbertson P, et al. Among authors: bujaroski rs. Biomolecules. 2022 Sep 16;12(9):1309. doi: 10.3390/biom12091309. Biomolecules. 2022. PMID: 36139148 Free PMC article.
An amiloride derivative is active against the F1Fo-ATP synthase and cytochrome bd oxidase of Mycobacterium tuberculosis.
Hards K, Cheung CY, Waller N, Adolph C, Keighley L, Tee ZS, Harold LK, Menorca A, Bujaroski RS, Buckley BJ, Tyndall JDA, McNeil MB, Rhee KY, Opel-Reading HK, Krause K, Preiss L, Langer JD, Meier T, Hasenoehrl EJ, Berney M, Kelso MJ, Cook GM. Hards K, et al. Among authors: bujaroski rs. Commun Biol. 2022 Feb 24;5(1):166. doi: 10.1038/s42003-022-03110-8. Commun Biol. 2022. PMID: 35210534 Free PMC article.
Automated Patch Clamp Screening of Amiloride and 5-N,N-Hexamethyleneamiloride Analogs Identifies 6-Iodoamiloride as a Potent Acid-Sensing Ion Channel Inhibitor.
Finol-Urdaneta RK, McArthur JR, Aboelela A, Bujaroski RS, Majed H, Rangel A, Adams DJ, Ranson M, Kelso MJ, Buckley BJ. Finol-Urdaneta RK, et al. Among authors: bujaroski rs. Mol Pharm. 2023 Jul 3;20(7):3367-3379. doi: 10.1021/acs.molpharmaceut.2c01083. Epub 2023 Jun 1. Mol Pharm. 2023. PMID: 37260417
Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride.
Buckley BJ, Aboelela A, Majed H, Bujaroski RS, White KL, Powell AK, Wang W, Katneni K, Saunders J, Shackleford DM, Charman SA, Cook GM, Kelso MJ, Ranson M. Buckley BJ, et al. Among authors: bujaroski rs. Bioorg Med Chem. 2021 May 1;37:116116. doi: 10.1016/j.bmc.2021.116116. Epub 2021 Mar 23. Bioorg Med Chem. 2021. PMID: 33799173