Design and synthesis of new donepezil analogs derived from arylpiperazine scaffold as acetylcholinesterase inhibitors
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, vol.196, no.3, pp.283-293, 2020 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 196 Issue: 3
- Publication Date: 2020
- Doi Number: 10.1080/10426507.2020.1830773
- Journal Name: PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Index Chemicus (IC)
- Page Numbers: pp.283-293
- Keywords: Thiazole, piperazine, anticholinesterase activity, acetylcholinesterase inhibition, molecular modeling, BUTYRYLCHOLINESTERASE, DERIVATIVES
- Anadolu University Affiliated: Yes
Abstract
Newly synthesized 4-substituted phenyl-2-(4-substituted phenylpiperazine-1-yl)thiazole derivatives (4a-v) were evaluated in terms of their acetylcholinesterase (AChE) inhibition activities. Twenty-two compounds were tested against AChE at six different concentrations that varied between 10(-4)and 10(-9) M. The concentrations that inhibited AChE were calculated between 1.15 and 3.45 mu M in seven compounds (4a,4b,4h,4l,4m,4q,4r). Compounds4m,4b, and4lrepresented 1.15, 1.31, 1.34 mu M (IC50) inhibitions, respectively. Although the inhibition values are lower than that of donepezil, they are considerable. Modeling studies of these analogs revealed similar positioning with donepezil, in which Ar-Ar interactions with Tyr337 and Trp 286 exist.