研究目的
To design, synthesize, and evaluate novel piperamides for antimicrobial and anticonvulsant activity, and to study their binding interaction with bovine serum albumin using fluorescence spectroscopy.
研究成果
The synthesized piperamides, particularly 8a and 8h, exhibit significant antimicrobial and anticonvulsant activities with lower toxicity compared to reference drugs. The binding interaction with BSA occurs through static quenching, with one binding site and specific binding constants and distances. These findings suggest potential for further development as therapeutic agents.
研究不足
The study is limited to in vitro and animal models; human trials are not conducted. The number of compounds tested is small, and the antimicrobial activity may vary with different strains. The binding studies are under imitated physiological conditions, which may not fully replicate in vivo environments.
1：Experimental Design and Method Selection:
The study involved the synthesis of piperamide derivatives through chemical reactions, evaluation of antimicrobial activity using agar disc diffusion and dilution methods, assessment of anticonvulsant activity via in vivo tests (MES and PTZ), and investigation of protein binding using fluorescence quenching and UV-vis spectroscopy. Theoretical models included Stern-Volmer equation and Forster energy transfer theory.
2：Sample Selection and Data Sources:
Synthesized compounds 8a-j were used as samples. Bacterial strains (S. aureus, B. subtilis, E. coli, P. aeruginosa) and fungal strains (A. flavus, C. albicans) were sourced for antimicrobial testing. Mice were used for anticonvulsant testing. Bovine serum albumin (BSA) was used for binding studies.
3：List of Experimental Equipment and Materials:
Chemicals included piperonal, malonic acid, piperidine, dimethylaluminium chloride, NaNO2, various alcohols, THF, DMSO-d6 for NMR, and BSA. Equipment: NMR spectrometer (400 MHz), IR spectrometer, mass spectrometer, fluorescence spectrometer, UV-vis spectrometer.
4：Experimental Procedures and Operational Workflow:
Synthesis involved multi-step reactions with specific conditions (e.g., reflux, stirring times). Antimicrobial activity was tested by agar disc diffusion and MIC determination. Anticonvulsant activity was assessed through MES and PTZ tests in mice. Binding studies involved titrating PA with BSA and measuring fluorescence intensity changes.
5：Data Analysis Methods:
Data were analyzed using statistical methods for MIC and pharmacological parameters (ED50, TD50). Fluorescence data were processed with Stern-Volmer plots and binding constant calculations.
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