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Synthesis and Evaluation of Phenoxybenzylpiperidinyl Analogues as Agonists of the Chemokine Receptor CCR8.

Chem Biodivers

September 2025

Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Molecular, Structural and Translational Virology Research Group, KU Leuven, Leuven, Belgium.

The human chemokine receptor 8 (CCR8) received attention as target for the treatment of various autoimmune disorders. Phenoxybenzylpiperidine analogues are known to act as CCR8 agonists, although their structure-activity relationship (SAR) has been studied to a limited extent. In this study, the SAR of phenoxybenzylpiperidinyl analogues was explored in a systematic way by fusion or insertion of various heterocyclic groups on the piperidinyl ring, yielding a set of 21 novel phenoxybenzylpiperidinyl derivatives.

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Design and Synthesis of Structurally Novel Acridospiroisoxazole Derivatives and Their Antifungal Activity Study.

Chem Biodivers

September 2025

Key Lab of Natural Product Chemistry and Application at Universities of Education, Department of Xinjiang Uygur Autonomous Region, School of Chemistry and Chemical Engineering, Yili Normal University, Xinjiang, China.

The persistent threat posed by phytopathogenic fungi to agricultural systems underscores the critical need for novel fungicides. Here, we synthesized and characterized a series of novel acridospiroisoxazole derivatives (H1-H36) using H/C NMR and mass spectrometry. The absolute configuration of compound H23 was confirmed using single-crystal x-ray diffraction analysis.

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Synthesis of Quaternary Ammonium Derivatives of Eugenol and Their Antifungal Mechanism against Wood-Decaying Fungi.

J Agric Food Chem

September 2025

College of Forestry, East China Woody Fragrance and Flavor Engineering Research Center of National Forestry and Grassland Administration; Jiangxi Provincial Key Laboratory of Improved Variety Breeding and Efficient Utilization of Native Tree Species, Jiangxi Agricultural University, Nanchang 330045,

To discover novel preservatives for treating wood-decaying fungi, 48 novel eugenol quaternary ammonium salt derivatives were designed and synthesized. Among them, compounds , , , , , , and showed remarkable antifungal activity against (), affording EC values ranging from 2.11-7.

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Replication of HIV-1 requires the coordinated action of host and viral transcription factors, most critically the viral transactivator Tat and the host nuclear factor κB (NF-κB). This activity is disrupted in infected cells that are cultured with extracellular vesicles (EVs) present in human semen, suggesting that they contain factors that could inform the development of new therapeutics. Here, we explored the contents of semen-derived EVs (SEVs) from uninfected donors and individuals with HIV-1 and identified host proteins that interacted with HIV Tat and the NF-κB subunit p65.

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Synthesis and Optical Properties of Unsymmetric Aromatically π-Extended BODIPY.

J Org Chem

September 2025

School of Chemical and Biopharmaceutical Sciences, Technological University Dublin, City Campus, Grangegorman, Dublin D07 EWV4, Ireland.

A series of unsymmetrically substituted BODIPY dyes featuring fused benzo- or naphtho-fragments on one pyrrolic unit were synthesized from the corresponding pyrrolic precursors. The synthetic route was optimized using a modular approach based on the condensation of formylpyrroles with alkylpyrroles, enabling the identification of precursor combinations that minimize byproduct formation and improve preparative yields. The resulting benzo- and naphtho-fused BODIPYs display intense fluorescence in the red region, with emission maxima spanning 590-680 nm and fluorescence quantum yields ranging from 0.

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