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Showing 1 to 5 of 5 for “"BAM15"”.
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Design and Synthesis of 8-Trifluoromethyl-Substituted Heterocyclic Small Molecule Mitochondrial Uncouplers for the Treatment of Metabolic Diseases
… take inspiration from the efficacious uncoupler, BAM15. BAM15 has proven to be effective against obesity, type 2 diabetes, liver disease, and several other conditions in animal models. However, BAM15 has not been in clinical trials due to its poor druglike properties, such as circulating drug …
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Design and Synthesis of Mitochondrial Uncouplers for the Treatment of Mitochondrial Dysfunction
… We use a potent and effective uncoupler, BAM15, as the basis for our design. BAM15 has been shown to effectively combat mitochondrial dysfunction in diseases models such as obesity. However, we are working on a redesign for improved druglike properties, such as half-life. Herein, we show …
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Structure-Activity Relationship Studies of Mitochondrial Uncouplers and PilB Inhibitors
… obesity models. Our previous work identified BAM15 (EC50 1.5 M) as a potent and efficacious mitochondrial uncoupler with potential for obesity treatment. In this study, we investigate in vitro and in vivo properties of hydroxylamine and hydrazine BAM15 derivatives and reveal the high …
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Complex Heterocycles as Mitochondrial Uncouplers
… of a small molecule mitochondrial uncoupler BAM15, which was efficacious in an obesity mouse model. Herein, we describe the design and synthesis of two scaffolds as well as their characterization as mitochondrial uncouplers through a series of in vitro and in vivo assays. Compounds that pass …
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Mitochondrial Uncouplers: Development as Therapeutics for Metabolic Diseases
Obesity and its comorbidities have emerged as serious healthcare concerns in the western world due to increased prevalence of nutritional overabundance and decreased physical activity. Due to the significant population affected and economic burden placed on national healthcare systems, there is a …