[HTML][HTML] An amiloride derivative is active against the F1Fo-ATP synthase and cytochrome bd oxidase of Mycobacterium tuberculosis

…, ZS Tee, LK Harold, A Menorca, RS Bujaroski… - Communications …, 2022 - nature.com
Increasing antimicrobial resistance compels the search for next-generation inhibitors with
differing or multiple molecular targets. In this regard, energy conservation in Mycobacterium …

[HTML][HTML] Screening of 5-and 6-substituted amiloride libraries identifies dual-uPA/NHE1 active and single target-selective inhibitors

BJ Buckley, A Kumar, A Aboelela, RS Bujaroski… - International Journal of …, 2021 - mdpi.com
The K + -sparing diuretic amiloride shows off-target anti-cancer effects in multiple rodent
models. These effects arise from the inhibition of two distinct cancer targets: the trypsin-like …

Automated Patch Clamp Screening of Amiloride and 5-N,N-Hexamethyleneamiloride Analogs Identifies 6-Iodoamiloride as a Potent Acid-Sensing Ion Channel …

…, JR McArthur, A Aboelela, RS Bujaroski… - Molecular …, 2023 - ACS Publications
Acid-sensing ion channels (ASICs) are transmembrane sensors of extracellular acidosis and
potential drug targets in several disease indications, including neuropathic pain and cancer …

[HTML][HTML] 6-furopyridine hexamethylene amiloride is a non-selective P2X7 receptor antagonist

…, RJ Turner, A Aboelela, H Majed, RS Bujaroski… - Biomolecules, 2022 - mdpi.com
P2X7 is an extracellular adenosine 5′-triphopshate (ATP)-gated cation channel present on
leukocytes, where its activation induces pro-inflammatory cytokine release and ectodomain …

Systematic evaluation of structure–property relationships and pharmacokinetics in 6-(hetero) aryl-substituted matched pair analogs of amiloride and 5-(N, N …

BJ Buckley, A Aboelela, H Majed, RS Bujaroski… - Bioorganic & Medicinal …, 2021 - Elsevier
The K + -sparing diuretic amiloride elicits anticancer activities in multiple animal models.
During our recent medicinal chemistry campaign aiming to identify amiloride analogs with …

[HTML][HTML] Antifungal activity of 6-substituted amiloride and hexamethylene amiloride (HMA) analogs

K Vu, BJ Buckley, RS Bujaroski, E Blumwald… - Frontiers in Cellular …, 2023 - frontiersin.org
Fungal infections have become an increasing threat as a result of growing numbers of
susceptible hosts and diminishing effectiveness of antifungal drugs due to multi-drug resistance. …

Automated patch clamp screening of amiloride and 5-N, N-hexamethyleneamiloride (HMA) analogs identifies 6-iodoamiloride as a potent acid-sensing ion channel …

…, JR McArthur, A Aboelela, RS Bujaroski… - bioRxiv, 2022 - biorxiv.org
Acid-sensing ion channels (ASICs) are transmembrane sensors of extracellular acidosis and
potential drug targets in several disease indications, including neuropathic pain and cancer …

A dual-targeting succinate dehydrogenase and F1Fo-ATP synthase inhibitor rapidly sterilizes replicating and non-replicating Mycobacterium tuberculosis

…, K Hards, LK Harold, A Aboelela, RS Bujaroski… - Cell Chemical …, 2023 - cell.com
Mycobacterial bioenergetics is a validated target space for antitubercular drug development.
Here, we identify BB2-50F, a 6-substituted 5-(N,N-hexamethylene)amiloride derivative as a …

Kinases in cerebral cavernous malformations: pathogenesis and therapeutic targets

C Qi, RS Bujaroski, J Baell, X Zheng - Biochimica et Biophysica Acta (BBA) …, 2023 - Elsevier
Cerebral cavernous malformations (CCMs) are low-flow, hemorrhagic vascular lesions of
the central nervous system of genetic origin, which can cause stroke-like symptoms and …

[CITATION][C] Bicyclic Acylguanidine Bioisosteres for Tuberculosis Indications

RS Bujaroski - 2022 - ro.uow.edu.au
"Bicyclic Acylguanidine Bioisosteres for Tuberculosis Indications" by Richard S. Bujaroski
Bujaroski, Richard S., Bicyclic Acylguanidine Bioisosteres for Tuberculosis Indications …