Antibacterial and Acetylcholinesterase Inhibitory Potentials of Triazenes Containg Sulfonamide Moiety
Bilginer, Sinan, Gul, Halise Inci, Hanci, Hayrunisa, Gulcin, Ilhami
The aim of this study was to investigate the antibacterial and acetylcholinesterase (AChE) inhibitory activities of 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl)benzenesulfonamides (compounds 1 - 12) and to find out new possible drug candidate molecules since the available agents in clinical use have some limitations. According to the results of antibacterial screening for compounds 1 - 12, most of the synthesized compounds were found to be effective against Gram-positive microorganisms while being ineffective (MIC > 1600 mu g/mL) on Gram-negative microorganisms. According to the AChE inhibition results, K-i values of compounds 1 - 12 were in the range of 5 +/- 1 - 34 +/- 2 nMtoward AChE. Tacrine (TAC) used as a reference drug had K-i value of 4 +/- 1 nM toward AChE. The non-substituted derivative compound 1 coluld be considered as a lead compound for this study in terms of AChE inhibitory activity, since its K-i value (5 +/- 1 nM) was close to that of the reference drug (TAC). Thus, compound 1 was docked at the binding site of AChE and showed good interaction with the target enzyme, suggesting their possible mechanism of action.
- Journal
- PHARMACEUTICAL CHEMISTRY JOURNAL
- Year
- 2021
- Volume
- 55
- Issue
- 3
- Pages
- 284-289
- ISSN
- 0091-150X
- eISSN
- 1573-9031
- DOI
- 10.1007/s11094-021-02412-1
- WoS UID
- WOS:000661364700006