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Published on: July 30, 2017
Antimicrobial and Anti-Inflammatory Activity of N-(2-Bromo-phenyl)-2-hydroxy-benzamide Derivatives and Their
Ioana Maria Carmen Ienașcu1,2, Adina Căta1, Antonina Evelina Lazăr1
1National Institute of Research and Development for Electrochemistry and Condensed Matter, 144 Dr. A. P. Podeanu, 300569 Timişoara, Romania.
Novel complexes of N-(2-bromo-phenyl)-2-hydroxy-benzamide derivatives and beta-cyclodextrin show enhanced antimicrobial and anti-inflammatory activities. Complexation with beta-cyclodextrin improved biological effects, demonstrating its potential for drug development.
Area of Science:
- Medicinal Chemistry
- Supramolecular Chemistry
Background:
- Novel complexes of N-(2-bromo-phenyl)-2-hydroxy-benzamide derivatives and beta-cyclodextrin were synthesized to enhance biological activity.
- Characterization involved spectral and thermal analyses to confirm complex formation.
Purpose of the Study:
- To evaluate the antimicrobial and in vitro anti-inflammatory activities of novel inclusion complexes.
- To determine the efficacy of complexation in enhancing the biological properties of the benzamide derivatives.
Main Methods:
- Inclusion complexes characterized using spectral and thermal analyses.
- Antimicrobial activity assessed via disk diffusion and minimum inhibitory concentration (MIC) methods.
- In vitro anti-inflammatory activity evaluated using protease inhibition assays.
Main Results:
- Supramolecular architectures indicated partial inclusion of benzamide derivatives within the cyclodextrin cavity.
- Compounds exhibited antimicrobial activity against Gram-positive bacteria (MIC = 2.5-5.0 mg/mL).
- Inhibition of trypsin activity was superior to acetylsalicylic acid (IC50 values: 0.04-0.07 mg/mL vs. 0.4051 ± 0.0026 mg/mL).
Conclusions:
- Complexation with beta-cyclodextrin significantly enhanced both antimicrobial and anti-inflammatory effects.
- The developed complexes show promise for therapeutic applications due to improved biological activity.
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