TY  - JOUR
TI  - Synthesis and pharmacological effects of novel benzenesulfonamides carrying
benzamide moiety as carbonic anhydrase and acetylcholinesterase inhibitors
AB  - N-(1-(4-Methoxyphenyl)-3-oxo-3-((4-(N-(substituted)sulfamoyl)phenyl)amino)prop-1-en-1-yl)benzamides 3a – g were
designed since sulfonamide and benzamide pharmacophores draw great attention in novel drug design due to their wide range of bioactivities including acetylcholinesterase (AChE) and human carbonic anhydrase I and II (hCA I and hCA II) inhibitory potencies.
Structure elucidation of the compounds was carried out by 1
H NMR, $^{13}C NMR$, and HRMS spectra. In vitro enzyme assays showed that
the compounds had significant inhibitory potential against hCA I, hCA II, and AChE enzymes at nanomolar levels. Ki values were in
the range of 4.07 ± 0.38 – 29.70 ± 3.18 nM for hCA I and 10.68 ± 0.98 – 37.16 ± 7.55 nM for hCA II while Ki values for AChE were in
the range of 8.91 ± 1.65 – 34.02 ± 5.90 nM. The most potent inhibitors 3g (Ki = 4.07 ± 0.38 nM, hCA I), 3c (Ki = 10.68 ± 0.98 nM, hCA
II), and 3f (Ki = 8.91 ± 1.65 nM, AChE) can be considered as lead compounds of this study with their promising bioactivity results.
Secondary sulfonamides showed promising enzyme inhibitory effects on AChE while primary sulfonamide derivative was generally effective on hCA I and hCA II isoenzymes.
AU  - Gulcin, ilhami
AU  - Tuğrak Sakarya, Mehtap
AU  - ANIL, BARIŞ
AU  - Gul, Halise Inci
DO  - 10.3906/kim-2007-37
PY  - 2020
JO  - Turkish Journal of Chemistry
VL  - 44
IS  - 6
SN  - 1300-0527
SP  - 1601
EP  - 1609
DB  - TRDizin
UR  - http://search/yayin/detay/524256
ER  -