Harmful fungus and the developed resistance to available fungicides seriously threaten the yield and quality of crops; thus, the search for new, highly efficient, and resistance-overcoming fungicides remains a quite urgent goal of agricultural scientists. In this study, a series of novel spiropyrimidinamine derivatives were designed and synthesized by employing the intermediate derivatization method (IDM). Their structures were identified by H NMR, elemental analyses, and MS spectra. The structure of compound was further confirmed by X-ray diffraction. Bioassays indicated that a number of the title compounds exhibited some fungicidal activities against . Especially, compound displayed excellent activity (EC = 0.422 mg/L), significantly higher than those of the commercialized fungicides cyazofamid, flumorph, and diflumetorim. The structure-activity relationship was also discussed. It was concluded that compound with super fungicidal potency and a novel structure is a promising agrochemical fungicide candidate for further development.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1021/acs.jafc.9b07055 | DOI Listing |
Arch Microbiol
January 2025
SLIIT, Malabe, Sri Lanka.
The development of new medicines with unique methods of antimicrobial action is desperately needed due to the emerging multidrug-resistant bacteria, such as methicillin-resistant Staphylococcus aureus. Therefore, antimicrobial peptoids have emerged as potential new antimicrobials. Thirteen peptoid analogues have been designed and synthesized via solid phase synthesis.
View Article and Find Full Text PDFACS Chem Neurosci
January 2025
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, 10 Center Drive, Bethesda, Maryland 20892, United States.
Receptor interacting protein kinase 1 (RIPK1) crucially upregulates necroptosis and is a key driver of inflammation. An effective PET radioligand for imaging brain RIPK1 would be useful for further exploring the role of this enzyme in neuroinflammation and for assisting drug discovery. Here, we report our progress on developing a PET radioligand for RIPK1 based on the phenyl-1-dihydropyrazole skeleton of a lead RIPK1 inhibitor, GSK'963.
View Article and Find Full Text PDFJ Drug Target
January 2025
Sunirmal Bhattacharjee, Bharat Pharmaceutical Technology, Amtali, Agartala, Tripura, India.
A significant area of computer science called artificial intelligence (AI) is successfully applied to the analysis of intricate biological data and the extraction of substantial associations from datasets for a variety of biomedical uses. AI has attracted significant interest in biomedical research due to its features: (i) better patient care through early diagnosis and detection; (ii) enhanced workflow; (iii) lowering medical errors; (v) lowering medical costs; (vi) reducing morbidity and mortality; (vii) enhancing performance; (viii) enhancing precision; and (ix) time efficiency. Quantitative metrics are crucial for evaluating AI implementations, providing insights, enabling informed decisions, and measuring the impact of AI-driven initiatives, thereby enhancing transparency, accountability, and overall impact.
View Article and Find Full Text PDFJ Phys Chem Lett
January 2025
Beijing National Laboratory for Molecular Science (BNLMS), State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
Clusters serve as the optimal model to elucidate the structure-property relationship of materials, bridging condensed matter and individual atoms. The pursuit of exceptionally stable clusters has garnered significant interest. The distinctive electronic configuration and symmetrical geometry generally provide a consistent rationale for their stability.
View Article and Find Full Text PDFUltrason Sonochem
December 2024
College of Biomass Science and Engineering and Healthy Food Evaluation Research Center, Sichuan University, Chengdu 610065, China. Electronic address:
Apple pectin (AP), a well-established dietary fiber, offers significant health benefits, particularly in immunomodulation. However, the structure-activity relationship (SAR) in this context remains poorly understood. This study aimed to elucidate the impact of varying degrees of esterification (DE) on AP's SAR in immunomodulatory activity.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!