Hacettepe University Journal of the Faculty of Pharmacy, Год журнала: 2024, Номер 44(3), С. 234 - 243
Опубликована: Авг. 9, 2024
In this study, N-((Z)-4-((3r,5r,7r)-adamantan-1-yl)-3-(3-amino-1,4-dioxo-1,4-dihydronaphthalen-2yl)thiazol-2(3H)-ylidene)-2,6-difluorobenzamide 3 was synthesized as a new 1,4-naphthoquinone thiazole hybrid compound by reaction of naphthoquinone acyl thiourea 2 with 1-((3r,5r,7r)-adamantan-1-yl)-2-bromoethan-1-one in 74% yield and its molecular structure characterized various analytical techniques such 1H/13C NMR, FT-IR, HRMS. The inhibition effect the on butyrylcholinesterase (BChE), acetylcholinesterase (AChE), human carbonic anhydrase isoenzymes (hCA I hCA II) investigated. product showed varying degrees 89.92 ± 10.47 nM (against I), 51.60 5.37 II), 68.11 6.58 AChE), 126.90 10.99 BChE). Although significant enzyme activity against enzymes tested, it higher AChE than standard drug Tacrine. Three acid dissociation constants (pKa) values (pKa1= 2.75±0.02, pKa2= 6.79±0.02, pKa3= 10.85±0.02) were determined potentiometrically 0.1 M NaCl ionic strength at 25.0±0.1 ºC 25% (v/v) DMSO:water hydro organic medium.
Язык: Английский