FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1992326577> ?p ?o ?g. }

• W1992326577 endingPage "95" @default.
• W1992326577 startingPage "82" @default.
• W1992326577 abstract "The design, synthesis, and pharmacological evaluation of donepezil–indolyl based amines 7–10, amides 12–16, and carboxylic acid derivatives 5 and 11, as multipotent ASS234 analogs, able to inhibit simultaneously cholinesterase (ChE) and monoamine oxidase (MAO) enzymes for the potential treatment of Alzheimer's disease (AD), is reported. Theoretical studies using 3D-Quantitative Structure–Activity Relationship (3D-QSAR) was used to define 3D-pharmacophores for inhibition of MAO A/B, AChE, and BuChE enzymes. We found that, in general, and for the same substituent, amines are more potent ChE inhibitors (see compounds 12, 13 versus 7 and 8) or equipotent (see compounds 14, 15 versus 9 and 10) than the corresponding amides, showing a clear EeAChE inhibition selectivity. For the MAO inhibition, amides were not active, and among the amines, compound 14 was totally MAO A selective, while amines 15 and 16 were quite MAO A selective. Carboxylic acid derivatives 5 and 11 showed a multipotent moderate selective profile as EeACE and MAO A inhibitors. Propargylamine 15 [N-((5-(3-(1-benzylpiperidin-4-yl)propoxy)-1-methyl-1H-indol-2-yl)methyl)prop-2-yn-1-amine] resulted in the most potent hMAO A (IC50 = 5.5 ± 1.4 nM) and moderately potent hMAO B (IC50 = 150 ± 31 nM), EeAChE (IC50 = 190 ± 10 nM), and eqBuChE (IC50 = 830 ± 160 nM) inhibitor. However, the analogous N-allyl and the N-morpholine derivatives 16 and 14 deserve also attention as they show an attractive multipotent profile. To sum up, donepezil–indolyl hybrid 15 is a promising drug for further development for the potential prevention and treatment of AD." @default.
• W1992326577 created "2016-06-24" @default.
• W1992326577 creator A5013717837 @default.
• W1992326577 creator A5018104052 @default.
• W1992326577 creator A5028704915 @default.
• W1992326577 creator A5039672667 @default.
• W1992326577 creator A5041836281 @default.
• W1992326577 creator A5044944147 @default.
• W1992326577 creator A5052444783 @default.
• W1992326577 creator A5070312790 @default.
• W1992326577 creator A5082905681 @default.
• W1992326577 creator A5086597259 @default.
• W1992326577 creator A5087613123 @default.
• W1992326577 date "2014-03-01" @default.
• W1992326577 modified "2023-09-27" @default.
• W1992326577 title "Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil–indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease" @default.
• W1992326577 cites W1550032904 @default.
• W1992326577 cites W1574019439 @default.
• W1992326577 cites W1940331911 @default.
• W1992326577 cites W1971048984 @default.
• W1992326577 cites W1980234111 @default.
• W1992326577 cites W1981775239 @default.
• W1992326577 cites W1998253336 @default.
• W1992326577 cites W1998700502 @default.
• W1992326577 cites W2000446523 @default.
• W1992326577 cites W2006734683 @default.
• W1992326577 cites W2007487695 @default.
• W1992326577 cites W2018863509 @default.
• W1992326577 cites W2024770800 @default.
• W1992326577 cites W2025204606 @default.
• W1992326577 cites W2025223727 @default.
• W1992326577 cites W2031580687 @default.
• W1992326577 cites W2033773654 @default.
• W1992326577 cites W2036755018 @default.
• W1992326577 cites W2038684398 @default.
• W1992326577 cites W2039069312 @default.
• W1992326577 cites W2039402692 @default.
• W1992326577 cites W2046827775 @default.
• W1992326577 cites W2047749116 @default.
• W1992326577 cites W2052811581 @default.
• W1992326577 cites W2054118966 @default.
• W1992326577 cites W2055380784 @default.
• W1992326577 cites W2058732924 @default.
• W1992326577 cites W2064086864 @default.
• W1992326577 cites W2064436235 @default.
• W1992326577 cites W2066251314 @default.
• W1992326577 cites W2071144635 @default.
• W1992326577 cites W2072219894 @default.
• W1992326577 cites W2089147516 @default.
• W1992326577 cites W2092539345 @default.
• W1992326577 cites W2092815169 @default.
• W1992326577 cites W2098655668 @default.
• W1992326577 cites W2100969363 @default.
• W1992326577 cites W2101919031 @default.
• W1992326577 cites W2118200955 @default.
• W1992326577 cites W2120586432 @default.
• W1992326577 cites W2131626361 @default.
• W1992326577 cites W2131697773 @default.
• W1992326577 cites W2135732933 @default.
• W1992326577 cites W2138645881 @default.
• W1992326577 cites W2142093490 @default.
• W1992326577 cites W2144135270 @default.
• W1992326577 cites W2145810295 @default.
• W1992326577 cites W2146158590 @default.
• W1992326577 cites W2152301430 @default.
• W1992326577 cites W2161809622 @default.
• W1992326577 cites W2162166182 @default.
• W1992326577 cites W2182593958 @default.
• W1992326577 cites W2302113434 @default.
• W1992326577 cites W2313968233 @default.
• W1992326577 cites W4242215325 @default.
• W1992326577 cites W4247225877 @default.
• W1992326577 doi "https://doi.org/10.1016/j.ejmech.2013.12.028" @default.
• W1992326577 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24530494" @default.
• W1992326577 hasPublicationYear "2014" @default.
• W1992326577 type Work @default.
• W1992326577 sameAs 1992326577 @default.
• W1992326577 citedByCount "105" @default.
• W1992326577 countsByYear W19923265772014 @default.
• W1992326577 countsByYear W19923265772015 @default.
• W1992326577 countsByYear W19923265772016 @default.
• W1992326577 countsByYear W19923265772017 @default.
• W1992326577 countsByYear W19923265772018 @default.
• W1992326577 countsByYear W19923265772019 @default.
• W1992326577 countsByYear W19923265772020 @default.
• W1992326577 countsByYear W19923265772021 @default.
• W1992326577 countsByYear W19923265772022 @default.
• W1992326577 countsByYear W19923265772023 @default.
• W1992326577 crossrefType "journal-article" @default.
• W1992326577 hasAuthorship W1992326577A5013717837 @default.
• W1992326577 hasAuthorship W1992326577A5018104052 @default.
• W1992326577 hasAuthorship W1992326577A5028704915 @default.
• W1992326577 hasAuthorship W1992326577A5039672667 @default.
• W1992326577 hasAuthorship W1992326577A5041836281 @default.
• W1992326577 hasAuthorship W1992326577A5044944147 @default.
• W1992326577 hasAuthorship W1992326577A5052444783 @default.
• W1992326577 hasAuthorship W1992326577A5070312790 @default.
• W1992326577 hasAuthorship W1992326577A5082905681 @default.

• next