Bioorganic Chemistry p. 393 - 404 (2019)
Update date:2022-08-11
Topics:
Bi?er, Abdullah
Taslimi, Parham
Yakal?, Gül
Gül?in, Ilhami
Serdar Gültekin, Mehmet
Turgut Cin, Günseli
In this study, a series of novel bis-thiomethylcyclohexanone compounds (3a–3j) were synthesized by the addition of thio-Michael to the bis-chalcones under mild reaction conditions. The bis-thiomethylcyclohexanone derivatives (bis-sulfides) were characterized by 1H NMR, 13C NMR, FTIR and elemental analysis techniques. Furthermore, the molecular and crystal structures of 3h, 3i and 3j compounds were determined by single crystal X-ray diffraction studies. In this study, X-ray crystallography provided an alternative and often-complementary means for elucidating functional groups at the enzyme inhibitory site. Acetylcholinesterase (AChE) is a member of the hydrolase protein super family and has a significant role in acetylcholine-mediated neurotransmission. Here, we report the synthesis and determining of novel bis-thiomethylcyclohexanone compounds based hybrid scaffold of AChE inhibitors. The newly synthesized bis-thiomethylcyclohexanone compounds showed Ki values of in range of 39.14–183.23 nM against human carbonic anhydrase I isoenzyme (hCA I), 46.03–194.02 nM against human carbonic anhydrase II isoenzyme (hCA II), 4.55–32.64 nM against AChE and 12.77–37.38 nM against butyrylcholinesterase (BChE). As a result, novel bis-thiomethylcyclohexanone compounds can have promising anti Alzheimer drug potential and record novel hCA I, and hCA II enzymes inhibitor.
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Doi:10.1021/ja303822c
(2012)Doi:10.1055/s-1984-30754
(1984)Doi:10.1039/jr9600003646
(1960)Doi:10.1016/0040-4039(95)01229-B
(1995)Doi:10.1002/ejoc.201701662
(2018)Doi:10.1246/bcsj.71.905
(1998)