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- W3146405454 abstract "The multifactorial nature of Alzheimer's disease (AD) is a reason for the lack of effective drugs as well as a basis for the development of multi-target-directed ligands (MTDLs). As cases increase in developing countries, there is a need of new drugs that are not only effective but also accessible. With this motivation, we report the first sustainable MTDLs, derived from cashew nutshell liquid (CNSL), an inexpensive food waste with anti-inflammatory properties. We applied a framework combination of functionalized CNSL components and well-established acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) tacrine templates. MTDLs were selected based on hepatic, neuronal, and microglial cell toxicity. Enzymatic studies disclosed potent and selective AChE/BChE inhibitors (5, 6, and 12), with subnanomolar activities. The X-ray crystal structure of 5 complexed with BChE allowed rationalizing the observed activity (0.0352 nM). Investigation in BV-2 microglial cells revealed antineuroinflammatory and neuroprotective activities for 5 and 6 (already at 0.01 μM), confirming the design rationale." @default.
- W3146405454 created "2021-04-13" @default.
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- W3146405454 date "2021-04-08" @default.
- W3146405454 modified "2023-10-17" @default.
- W3146405454 title "Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer’s Disease" @default.
- W3146405454 cites W1503006786 @default.
- W3146405454 cites W1577520625 @default.
- W3146405454 cites W1581222683 @default.
- W3146405454 cites W1592483428 @default.
- W3146405454 cites W1793575896 @default.
- W3146405454 cites W1965300654 @default.
- W3146405454 cites W1965910452 @default.
- W3146405454 cites W1966728055 @default.
- W3146405454 cites W1969451266 @default.
- W3146405454 cites W1971048984 @default.
- W3146405454 cites W1971513938 @default.
- W3146405454 cites W1977774397 @default.
- W3146405454 cites W1981775239 @default.
- W3146405454 cites W1985026267 @default.
- W3146405454 cites W1995024816 @default.
- W3146405454 cites W2003674452 @default.
- W3146405454 cites W2005447026 @default.
- W3146405454 cites W2013176372 @default.
- W3146405454 cites W2026976753 @default.
- W3146405454 cites W2028733293 @default.
- W3146405454 cites W2031299209 @default.
- W3146405454 cites W2031391963 @default.
- W3146405454 cites W2032753543 @default.
- W3146405454 cites W2033591223 @default.
- W3146405454 cites W2044632501 @default.
- W3146405454 cites W2062159889 @default.
- W3146405454 cites W2062533676 @default.
- W3146405454 cites W2063249182 @default.
- W3146405454 cites W2080946103 @default.
- W3146405454 cites W2087243986 @default.
- W3146405454 cites W2089388005 @default.
- W3146405454 cites W2098167941 @default.
- W3146405454 cites W2098437204 @default.
- W3146405454 cites W2104182950 @default.
- W3146405454 cites W2112006614 @default.
- W3146405454 cites W2119895789 @default.
- W3146405454 cites W2122429894 @default.
- W3146405454 cites W2124026197 @default.
- W3146405454 cites W2128627731 @default.
- W3146405454 cites W2128671521 @default.
- W3146405454 cites W2139815913 @default.
- W3146405454 cites W2146249493 @default.
- W3146405454 cites W2147180300 @default.
- W3146405454 cites W2152161559 @default.
- W3146405454 cites W2158603760 @default.
- W3146405454 cites W2163341755 @default.
- W3146405454 cites W2180229411 @default.
- W3146405454 cites W2193637546 @default.
- W3146405454 cites W2206696478 @default.
- W3146405454 cites W2329696749 @default.
- W3146405454 cites W2335925695 @default.
- W3146405454 cites W2336534940 @default.
- W3146405454 cites W2343878936 @default.
- W3146405454 cites W2463644552 @default.
- W3146405454 cites W2520082135 @default.
- W3146405454 cites W2542856291 @default.
- W3146405454 cites W2585093856 @default.
- W3146405454 cites W2603221479 @default.
- W3146405454 cites W2603474936 @default.
- W3146405454 cites W2609990777 @default.
- W3146405454 cites W2765584833 @default.
- W3146405454 cites W2773982889 @default.
- W3146405454 cites W2774623109 @default.
- W3146405454 cites W2782618472 @default.
- W3146405454 cites W2808183585 @default.
- W3146405454 cites W2890186102 @default.
- W3146405454 cites W2911848688 @default.
- W3146405454 cites W2912275633 @default.
- W3146405454 cites W2931752016 @default.
- W3146405454 cites W2945427404 @default.
- W3146405454 cites W2945796574 @default.
- W3146405454 cites W2951638914 @default.
- W3146405454 cites W2966431778 @default.
- W3146405454 cites W2980601903 @default.
- W3146405454 cites W2999699157 @default.
- W3146405454 cites W3006710361 @default.
- W3146405454 cites W3034113709 @default.