Herein, a new series of -substituted 1,2,3-triazolylmethyl indole derivatives 4(a-u) was synthesized by rationally incorporating a pharmacophoric active heterocyclic ring containing indole and triazole moieties in one molecular frame the conventional and microwave irradiation methods. Briefly, the new compounds 4(a-u) were synthesized the -alkylation of tetrahydro-1-carbazoles followed by click reaction and copper-catalyzed Huisgen [3 + 2] cycloaddition in the presence of copper sulphate and sodium ascorbate with various aromatic azides 3(a-m). All the newly synthesized compounds were characterized H and C NMR, mass, and IR spectroscopy and evaluated for their antimicrobial, antioxidant and anticancer activities. Among the synthesized compounds, 4d, 4j, 4n, 4p, 4s and 4r were found to exhibit good antimicrobial, antioxidant, anticancer activities. The biological activity of the synthesized compounds was further supplemented by molecular docking studies against the target receptors caspase-3 and 17-beta-hydroxy steroid dehydrogenase type 1, revealing that the reported structures best fit into the active site pocket of the target molecules.
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http://dx.doi.org/10.1039/d2ra05960f | DOI Listing |
NPJ Biofilms Microbiomes
December 2024
Costerton Biofilm Center, Department of Immunology and Microbiology, University of Copenhagen, Copenhagen, 2200, Denmark.
The evolution of antimicrobial resistance (AMR) in biofilms, driven by mechanisms like oxidative stress, is a major challenge. This study investigates whether antioxidants (AOs) such as N-acetyl-cysteine (NAC) and Edaravone (ED) can reduce AMR in Pseudomonas aeruginosa biofilms exposed to sub-inhibitory concentrations of ciprofloxacin (CIP). In vitro experimental evolution studies were conducted using flow cells and glass beads biofilm models.
View Article and Find Full Text PDFNat Commun
December 2024
Peking University People's Hospital, Peking University Institute of Hematology, National Clinical Research Center for Hematologic Disease, Beijing Key Laboratory of Hematopoietic Stem Cell Transplantation, Collaborative Innovation Center of Hematology, Peking University, Beijing, China.
Although acute myeloid leukemia (AML) affects hematopoietic stem cell (HSC)-supportive microenvironment, it is largely unknown whether leukemia-modified bone marrow (BM) microenvironment can be remodeled to support normal hematopoiesis after complete remission (CR). As a key element of BM microenvironment, endothelial progenitor cells (EPCs) provide a feasible way to investigate BM microenvironment remodeling. Here, we find reduced and dysfunctional BM EPCs in AML patients, characterized by impaired angiogenesis and high ROS levels, could be partially remodeled after CR and improved by N-acetyl-L-cysteine (NAC).
View Article and Find Full Text PDFJ Pediatr Hematol Oncol
January 2025
Departments of Pediatric Hematology.
Congenital thrombotic thrombocytopenic purpura (cTTP), which is associated with mutations in the gene for a disintegrin and metalloproteinase with a thrombospondin type 1 motif member 13 (ADAMTS13), is a chronic and lifelong disease. The clinical course is variable. Regularly using ADAMTS13-containing products such as fresh frozen plasma (FFP) for long-term prophylaxis is the most important treatment to prevent thrombotic microangiopathy (TMA) episodes.
View Article and Find Full Text PDFPharm Dev Technol
December 2024
Department of Cariology, Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, India.
The increasing prevalence of dental pathogens and oral cancer calls for new therapeutic agents. Nanoparticle (NPs) based tumor therapy enables precise targeting and controlled drug release, improving anti-cancer treatment efficacy while reducing systemic toxicity. Zinc oxide NPs (ZnO NPs) are notable in nanomedicine for their exceptional physicochemical and biological properties.
View Article and Find Full Text PDFPeerJ
December 2024
College of Coastal Agricultural Sciences, Guangdong Ocean University, Zhanjiang, Guangdong, China.
Soil salinization has resulted in a significant decrease in crop yields, particularly affecting the production of crops like rice ( L.). Prohexadione calcium (Pro-Ca) can enhance crop resilience against failure by managing plant height.
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