A novel series of medium size (S)-3-alkyl-3,4,6,7-tetrahydro-1H-benzo[e][1,4]diazonine-2,5-dione analogues were synthesized from (E)-3-(2-nitrophenyl)acrylicacid reacting with various amino acid esters using Di-isopropyl Carbodiimide as a coupling agent. The final cyclization is carried out by using reagent 1-Ethyl-3(3-dimethylaminopropyl) Carbodiimide Hydrochloride. The synthesized compounds have been supported by Mass, H-NMR and C-NMR. Further antibacterial studies were conducted, where some molecules are noticed with potent activity, especially molecule shown highest activity which was also supported by molecular docking studies. All final molecules were docked with enzyme peptide deformylase to determine the probable binding conformation.
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http://dx.doi.org/10.17179/excli2017-193 | DOI Listing |
Int J Nanomedicine
January 2025
School of Pharmacy, Jiangxi Medical College, Nanchang University, Nanchang, 330006, People's Republic of China.
Purpose: To improve the oral absorption of relugolix (RLGL), which has low oral bioavailability due to its low solubility and being a substrate of P-glycoprotein (P-gp). A solid self-microemulsifying drug delivery system of relugolix (RLGL-S-SMEDDS) was prepared and evaluated in vitro and in vivo.
Methods: The composition of the solid self-microemulsifying drug delivery system (S-SMEDDS) was selected by solubility study and pseudo-ternary phase diagram, and further optimized by Design-Expert optimization design.
Phys Chem Chem Phys
January 2025
Centre for Surface Science, Physical Chemistry Section, Department of Chemistry, Jadavpur University, Kolkata-700032, West Bengal, India.
The complexation behavior and binding affinity of Triton X-100 (TX-100) and Triton X-114 (TX-114) with β-cyclodextrin (β-CD) were extensively studied in an aqueous medium using a comprehensive suite of experimental techniques. These techniques allowed for the evaluation of key physicochemical parameters, including critical micelle concentration (cmc), aggregation number (), Stern-Volmer constant, and particle size distribution. These metrics were instrumental in understanding the underlying mechanism of the host-guest interaction between β-CD and Triton-X.
View Article and Find Full Text PDFEnviron Res
January 2025
School of Life Science and Engineering, Southwest University of Science and Technology,Mianyang 621010, Sichuan, P.R. China; Engineering Research Center of Biomass Materials, Ministry of Education, Southwest University of Science and Technology, Mianyang 621010, Sichuan, P. R. China. Electronic address:
Microplastic (MP) pollution has become one of global concern. While MP pollution in lakes has been well studied, research on MP sources, distribution, and ecological risks in the Tibetan Plateau is limited. We systematically investigated the MP abundance and distribution in alpine travertine lakes in Jiuzhai nature reserve located in east edge of Qinghai-Tibetan Plateau and assessed the distributions of microbiomes, antibiotic resistance genes (ARGs), and virulence factor genes (VFGs) in water, sediments, and MPs, using macrogenomics.
View Article and Find Full Text PDFClin Microbiol Infect
January 2025
European Society of Clinical Microbiology and Infectious Diseases Study Group on Clostridioides difficile (ESGCD); Experimental Bacteriology Research Group, Leiden University Center for Infectious Diseases (LUCID), Leiden University Medical Center, Leiden, The Netherlands. Electronic address:
Objectives: Increasing resistance to antimicrobials used for the treatment of Clostridioides difficile infections necessitates reproducible antimicrobial susceptibility testing. Current guidelines take a one-size-fits-all approach and/or offer limited guidance. We investigated how the choice of medium affects measured MIC values across two sites.
View Article and Find Full Text PDFJMIR Public Health Surveill
January 2025
Monitoring, Evaluation, and Learning Platform USAID, Jakarta, Indonesia.
Background: Indonesia's vast archipelago and substantial population size present unique challenges in addressing its multifaceted HIV epidemic, with 90% of its 514 districts and cities reporting cases. Identifying key populations (KPs) is essential for effectively targeting interventions and allocating resources to address the changing dynamics of the epidemic.
Objective: We examine the 2022 mapping of Indonesia's KPs to develop improved HIV and AIDS interventions.
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