Akademik Veri Yönetim Sistemi
PHARMACEUTICAL CHEMISTRY JOURNAL, cilt.55, sa.3, ss.284-289, 2021 (SCI-Expanded)
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.