A diverse set of 4,7-dihydro-[1,2,3]thiadiazolo[5,4-b]pyridine-6-carboxamides 4(a-o) was synthesized via a one-pot reaction of 5-amino-[1,2,3]thiadiazole, various aromatic aldehydes, and different acetoacetanilides, using glacial acetic acid. The resulting compounds were obtained in moderate to good yields. All the newly synthesized compounds were evaluated for their antimicrobial activity. Among them, compound 4 e demonstrated superior efficacy against the Salinivibrio proteolyticus strain of Gram-negative bacteria compared to ciprofloxacin. Compound 4 d exhibited the highest potency against the fungal strain Candida albicans, surpassing amphotericin B. The physicochemical characteristics of 4 d and 4 e were assessed. According to docking analysis, DHTDAPy 4 e shows a higher binding affinity of -7.2 kcal/mol in the binding cavity of the receptor. These findings illustrate the safety, tolerability, and potency of the newly synthesized DHTDAPy compounds against fungal and bacterial infections.
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http://dx.doi.org/10.1002/cmdc.202400595 | DOI Listing |
RSC Adv
January 2025
University of Split, Faculty of Science, Department of Chemistry R. Bošković 33 Split Croatia
Quaternary ammonium compounds (QACs) have served as essential antimicrobial agents for nearly a century due to their rapid membrane-disrupting action. However, the emergence of bacterial resistance and environmental concerns have driven interest in alternative designs, such as "soft QACs", which are designed for enhanced biodegradability and reduced resistance potential. In this study, we explored the antibacterial properties and mechanisms of action of our newly synthesized soft QACs containing a labile amide bond within a quinuclidine scaffold.
View Article and Find Full Text PDFRSC Adv
January 2025
Department of Chemistry, Faculty of Science (Boys), Al-Azhar University 11884 Nasr City Cairo Egypt
Herein, novel thiazolo[4,5-]quinoxalin-2-ones 2-6 and thiazolo[4,5-]quinoxalin-2(3)-imines 7-9 were synthesized and characterized using elemental analysis, IR spectroscopy, and H/C NMR to confirm their structures. The efficacy of the newly designed thiazolo-quinoxalines 2, 3, 4, 5, 7, 8, and 9 against the cotton leafworm (2nd and 4th instar larvae) was evaluated, and results revealed insecticidal activity with variable and good mortality percentages. A SAR study was also discussed.
View Article and Find Full Text PDFSmall
January 2025
Institute of Multidisciplinary Research for Advanced Materials (IMRAM), Tohoku University, Sendai, 980-8577, Japan.
Hollandite-type α-MnO exhibits exceptional promise in current industrial applications and in advancing next-generation green energy technologies, such as multivalent (Mg, Ca, and Zn) ion battery cathodes and aerobic oxidation catalysts. Considering the slow diffusion of multivalent cations within α-MnO tunnels and the catalytic activity at edge surfaces, ultrasmall α-MnO particles with a lower aspect ratio are expected to unlock the full potential. In this study, ultrasmall α-MnO (<10 nm) with a low aspect ratio (c/a ≈ 2) is synthesized using a newly developed alcohol solution process.
View Article and Find Full Text PDFCommun Chem
January 2025
National Institute of Chemistry, Hajdrihova 19, SI-1001, Ljubljana, Slovenia.
Iminophosphoranes with the general formula (RP═NR') have great potential in synthetic chemistry as valuable precursors/intermediates in organic synthesis or as building blocks for various organic compounds. However, the synthetic approaches and conditions to prepare iminophosphoranes are still poorly understood, limiting the utility of this chemistry for organic materials. In this article, a simple and efficient synthesis of previously unattainable poly(arylene iminophosphoranes) is reported.
View Article and Find Full Text PDFNat Commun
January 2025
Laboratory of Epigenome Integrity, Epigenetics & Cell Fate Centre, UMR7216 CNRS, Université Paris Cité, Paris, France.
The faithful segregation of intact genetic material and the perpetuation of chromatin states through mitotic cell divisions are pivotal for maintaining cell function and identity across cell generations. However, most exogenous mutagens generate long-lasting DNA lesions that are segregated during mitosis. How this segregation is controlled is unknown.
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