Adam S. Duerfeldt

Phenotypic Effects of a Small Molecule CpxA Phosphatase Inhibitor on Uropathogenic Escherichia coli

Alexis M. Stoorza, Erin E. Carlson, Adam S. Duerfeldt

Patients suffering from Urinary Tract Infections (UTIs) are faced with multidrug resistance and a lack of treatment options. An alternative strategy to traditional bactericidal drug design is to disarm pathogenic bacteria by targeting the regulation of virulence factors. Small-molecule CpxRA phosphatase inhibitor …

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Synthesis of a Carbon‐Linked Acyldepsipeptide Derivative

Katelyn G. Stevens-Davis, Xiaozheng Dou, Bo Hu, Yangxiong Li et autres

We report the synthesis and conformational analysis of a methylene‐linked acyldepsipeptide (ADEP). The convergent approach hinged on the generation of a protected vinylglycine synthon, a versatile noncanonical amino acid building block. A rationally optimized Grubbs metathesis and a new mode for macrocyclization …

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Development and Characterization of a Noncovalent Stimulator of Interferon Genes Proteolysis‐Targeting Chimeras

Bo Hu, Adam S. Duerfeldt

The cyclic GMP‐AMP synthase (cGAS)‐stimulator of interferon genes (STING) pathway activates the immune response upon detection of cytosolic dsDNA and is a key regulator of innate immunity. Overactivation of cGAS‐STING has been implicated in numerous inflammatory diseases, and inhibition of cGAS‐STING signaling …

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Oral Pharmacokinetic Evaluation of a Microemulsion-Based Delivery System for Novel A190 Prodrugs

Sagun Poudel, Chaolong Qin, Rudra Pangeni, Ziwei Hu et autres

Peroxisome proliferator-activated receptor alpha (PPARα) is a key regulator of lipid metabolism, making its agonists valuable therapeutic targets for various diseases, including chronic peripheral neuropathy. Existing PPARα agonists face limitations such as poor selectivity, sub-optimal bioavailability, and safety concerns. We previously demonstrated …

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Sustained release of a novel non-fibrate PPARα agonist from microparticles for neuroprotection in murine models of age-related macular degeneration

Yi Cui, Sagun Poudel, Nuo Xu, Kelu Zhou et autres

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New PPARα Agonist A190-Loaded Microemulsion for Chemotherapy-Induced Peripheral Neuropathy

Rudra Pangeni, Surendra Poudel, Sara M Herz, Grant Berkbigler et autres

Chemotherapy-induced peripheral neuropathy (CIPN) is a serious side effect of anticancer agents with limited effective preventive or therapeutic interventions. Although fenofibrate, a peroxisome proliferator-activated receptor-alpha (PPARα) agonist, has demonstrated neuroprotective and analgesic properties, its clinical utility is hindered by low receptor affinity, …

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Semisynthetic Tetramate-Containing Fungal Metabolites with Activity against Trichomonas vaginalis and Mycoplasma genitalium

Thilini Peramuna, Gwendolyn E. Wood, Ziwei Hu, Karen Wendt et autres

Tetramic acid-containing natural products are well known for their promising biological activity against various diseases. In our previous study, we reported fungal-derived tetramic acid-containing natural products with activity against Trichomonas vaginalis . Here, we demonstrate that Mycoplasma genitalium is also highly susceptible …

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Design and Assessment of First-Generation Heterobifunctional PPARα/STING Modulators

Bo Hu, Yi Cui, Julia Lee, Jian‐xing Ma et autres

Inflammatory retinal diseases such as diabetic retinopathy (DR) and age-related macular degeneration (AMD) are prominent causes of blindness in industrialized countries. The complexity of these diseases, involving diverse cell types and pathways that give rise to a multifactorial pathogenesis, complicates drug discovery. …

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Guiding the Way: Traditional Medicinal Chemistry Inspiration for Rational Gram-Negative Drug Design

Alexis M. Stoorza, Adam S. Duerfeldt

The discovery and development of small-molecule therapeutics effective against Gram-negative pathogens are highly challenging tasks. Most compounds that are active in biochemical settings fail to exhibit whole-cell activity. The major reason for this lack of activity is the effectiveness of bacterial cell …

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Correction to “Structure–Uptake Relationship Studies of Oxazolidinones in Gram-Negative ESKAPE Pathogens”

Ziwei Hu, Inga V. Leus, Brinda Chandar, Bradley Sherborne et autres

ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to "Structure–Uptake Relationship Studies of Oxazolidinones in Gram-Negative ESKAPE Pathogens"Ziwei HuZiwei HuMore by Ziwei Hu, Inga V. LeusInga V. LeusMore by Inga V. Leus, Brinda ChandarBrinda ChandarMore by Brinda Chandar, Bradley S. SherborneBradley …

Author Correction: Property space mapping of Pseudomonas aeruginosa permeability to small molecules

Inga V. Leus, Jon W. Weeks, Vincent Bonifay, Yue Shen et autres

The original version of this Article contained an error in the spelling of the author Dinesh Nath which was incorrectly given as Dinesh Nash.

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Design, Synthesis, and Structure–Activity Relationships of Biaryl Anilines as Subtype-Selective PPAR-alpha Agonists

Julia Lee, Ziwei Hu, Yuhong Anna Wang, Dinesh Nath et autres

The role of peroxisome proliferator-activated receptor alpha (PPARα) in retinal biology is clarifying, and evidence demonstrates that novel PPARα agonists hold promising therapeutic utility for diseases like diabetic retinopathy and age-related macular degeneration. Herein, we disclose the design and initial structure–activity relationships …

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