Though succinate dehydrogenase inhibitors (SDHIs) are quite successful in the modern agrochemical industry, the Fungicide Resistance Action Committee has classified the resistance risk as "medium to high". Structural analysis reveals that these antifungal chemotypes are highly conserved with amides as a consistent feature. This chemical factor may be a potential factor for the ever-increasing resistance risk. Introducing new antifungal structures or models may be a potent method to tackle this and find new bioactive compounds. In this Perspective, the recent progress in SDHIs without amide functionality from either synthetic endeavors or natural sources is showcased, focusing on their biological activities and a brief introduction of their mechanism. Synthetic advances in complex natural products are discussed, aiming to inspire new pharmaceutical discoveries and efficient synthesis methods. The challenges and strategies for the development of SDHIs are also discussed. This may offer insights for developing new SDHIs or chemical entities to combat the increasing resistance to commercial agrochemicals.
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http://dx.doi.org/10.1021/acs.jmedchem.4c02757 | DOI Listing |
Pest Manag Sci
January 2025
College of Materials and Chemistry and School of Plant Protection, Anhui Agricultural University, Hefei, China.
Background: Development of novel chiral antifungal agents for effective control of plant pathogens is urgently needed. In this study, a series of pyrazol-5-yl-benzamide derivatives containing chiral oxazoline moiety were rationally designed and developed based on molecular docking.
Results: The in vitro antifungal assay results indicated that compounds (rac)-4h (R = Et), (S)-4 h (R = S-Et) and (R)-4 h (R = R-Et) exhibited remarkable antifungal activities against Valsa mali with median effective concentration (EC) values of 0.
Biotech Histochem
January 2025
Faculty of Medicine Novi Sad, Department of Histology and Embriology, University of Novi Sad, Novi Sad, Serbia.
Numerous studies reported about potential effects of L-carnosine in regulation of tumor growth and metabolism. We evaluated the effects of different concentrations of L-carnosine from supplement on mitochondrial respiratory chain complexes of human embryo lung fibroblasts (MRC-5) and human breast cancer cells (MCF-7), with different energy pathways. Also, we analyzed the proliferation index and expression of various markers of oxidative stress.
View Article and Find Full Text PDFInflammation
January 2025
Department of Respiratory Medicine, Shenzhen Longhua District Central Hospital, Shenzhen, 518110, China.
Macrophages exhibit diverse phenotypes depending on environment status, which contribute to physiological and pathological processes of immunological diseases, including sepsis, asthma, multiple sclerosis and colitis. The alternative activation of macrophages is tightly regulated to avoid excessive activation and damage of tissues and organs. Certain works characterized that succinate dehydrogenase (SDH) altered function of macrophages and promoted inflammatory response in M1 macrophages via mitochondrial reactive oxygen species (ROS).
View Article and Find Full Text PDFItaconate is an immunomodulatory metabolite that alters mitochondrial metabolism and immune cell function. This organic acid is endogenously synthesized via tricarboxylic acid (TCA) metabolism downstream of TLR signaling. Itaconate-based treatment strategies are being explored to mitigate numerous inflammatory conditions.
View Article and Find Full Text PDFAnimals (Basel)
December 2024
College of Fisheries, Southwest University, Chongqing 402460, China.
Schizothoracine fishes in saltwater lakes of the Tibetan Plateau are important models for studying the evolution and uplift of the Tibetan Plateau. Examining their adaptation to the high-salt environment is interesting. In this study, we first assembled the RNA-Seq data of each tissue of , , and from Qinghai Lake, Selincuo Lake, and Namtso Lake, respectively, obtained by the group previously.
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