Design, Synthesis, and Biological Evaluation of [1,2,5]Oxadiazolo[3,4-]pyridin-7-ol as Mitochondrial Uncouplers for the Treatment of Obesity and Metabolic Dysfunction-Associated Steatohepatitis.

Mitochondrial uncouplers are small molecule protonophores that act to dissipate the proton motive force independent of adenosine triphosphate (ATP) synthase. Mitochondrial uncouplers such as BAM15 increase respiration and energy expenditure and have potential in treating a variety of metabolic diseases. In this study, we disclose the structure-activity relationship profile of 6-substituted [1,2,5]oxadiazolo[3,4-]pyridin-7-ol derivatives of BAM15.

Design, synthesis, and biological evaluation of imidazo[4,5-b]pyridine mitochondrial uncouplers for the treatment of metabolic dysfunction-associated steatohepatitis (MASH).

Small molecule mitochondrial uncouplers have gained traction for their potential therapeutic use against metabolic dysfunction-associated steatohepatitis (MASH). Herein, we report a novel imidazo[4,5-b]pyridine scaffold derived from iterative modifications of the potent uncoupler BAM15. Our structure-activity relationship (SAR) study demonstrated that this promising scaffold has a range of tolerated substitutions that allows for the modulation of uncoupling activity and in vivo pharmacokinetic properties.

Para-Methoxybenzylidene Acetal-Protected D-Glucosamine Derivatives as pH-Responsive Gelators and Their Applications for Drug Delivery.

Carbohydrate-based low molecular weight gelators (LMWGs) are compounds with the capability to self-assemble into complex molecular networks within a solvent, leading to solvent immobilization. This process of gel formation depends on noncovalent interactions, including Van der Waals, hydrogen bonding, and π-π stacking. Due to their potential applications in environmental remediation, drug delivery, and tissue engineering, these molecules have emerged as an important area of research.

Low-calorie diet induced weight loss may alter regulatory hormones and contribute to rebound visceral adiposity in obese persons with a family history of type-2 diabetes.

Purpose: To examine potential detrimental long-term effects of acute diet-induced weight loss on visceral adiposity, insulin resistance, cortisol, and adipokines in obese individuals at risk for type-2 diabetes.

Data Sources: Anthropometric measures (height, weight, waist circumference), self-report instruments, abdominal computed tomography (CT) scan, and blood samples (glucose, insulin, interleukin-6, leptin, adiponectin) were obtained from a convenience sample of 20 participants at baseline, after a 28-day low-calorie diet (800 kcal/day) intervention, and again 6 months later.

Conclusions: Fifteen of 20 participants completed the 28-day diet intervention and had a mean weight loss of 15 pounds.