1,4-Substituted 4-(1H)-pyridylene-hydrazone-type inhibitors of AChE, BuChE, and amyloid-β aggregation crossing the blood–brain barrier

Prinz, Michaela; Parlar, Sülünay; Bayraktar, Gülşah; Alptüzün, Vildan; Erciyas, Erçin; Fallarero, Adyary; Karlsson, Daniela; Vuorela, Pia; Burek, Małgorzata; Förster, Carola; Turunç, Ezgi; Armağan, Güliz; Yalçın, Ayfer; Schiller, Carola; Leuner, Kristina; Krug, Manuel; Sotriffer, Christoph A.; Holzgrabe, Ulrike

doi:10.1016/j.ejps.2013.04.024

Cited by 29 publications

(39 citation statements)

References 73 publications

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“…The inhibitory results (IC 50 value) against AChE and BuChE using SAC, SAC methyl ester derivatives (1-6), and SAC IPA ester derivatives (7)(8)(9)(10)(11)(12) are shown in Table 1. The parent compounds (SAC, ALA, and polyphenols) did not show any inhibitory activity against ChEs.…”

Section: Resultsmentioning

confidence: 99%

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(S)‐Allyl Cysteine Derivatives as a New‐type Cholinesterase Inhibitor

Kim

Lee

Jang

et al. 2015

Bulletin Korean Chem Soc

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Even though cholinesterase (ChE) inhibitors and N-methyl-D-aspartate (NMDA) receptor antagonist are clinically approved to treat Alzheimer's disease (AD) patients, new therapeutic compounds still need to be developed. Therefore, many new targets and novel anti-AD drugs targeting them have been developed. As inhibition of ChE is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort to identify new types of cholinergic drugs, S-allyl cysteine (SAC), which is the major ingredient of aged-garlic extract (AGE), was coupled with natural antioxidants. As SAC derivatives showed butyrylcholinesterase (BuChE) inhibitory activity, they constitute a new class of inhibitors for ChE and can be used as a novel natural-compounds-derived drug to treat AD patients.

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Section: Resultsmentioning

confidence: 99%

“…However, there was a significant improvement in BuChE inhibition. BuChE inhibitory values (IC 50 value) between SAC methyl esters (1-6) and SAC IPA esters (7)(8)(9)(10)(11)(12) are compared in Figure 3. SAC IPA ester (7) itself showed better inhibitory activity than SAC methyl ester (1) against BuChE.…”

Section: Resultsmentioning

confidence: 99%

(S)‐Allyl Cysteine Derivatives as a New‐type Cholinesterase Inhibitor

Kim

Lee

Jang

et al. 2015

Bulletin Korean Chem Soc

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“…[6][7][8][9][10] In the past years, many research groups have pursued the development of multi-target antiAlzheimer drugs as an advantageous approach over multi-target multi-drug strategies (drug cocktails and fixed-dose combinations). [11][12][13][14][15] Multi-target compounds have been usually designed to hit at least Aβ formation and aggregation and AChE activity, 16 especially prompted by the finding that AChE can bind Aβ, thereby promoting its aggregation and increasing its neurotoxicity. [17][18][19] The recognition site of Aβ within AChE is the so-called peripheral anionic site (PAS) and it is located at the entrance of a 20 Å deep narrow gorge that leads to the catalytic anionic site (CAS).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Multitarget Biological Profiling of a Novel Family of Rhein Derivatives As Disease-Modifying Anti-Alzheimer Agents

et al. 2014

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“…Due to the costliness of 40 and 42 residue b-amyloids, the research group of Holzgrabe developed a smaller peptide which contained 11 amino acids and possessed the same features in respect of fibril formation (Alptuzun et al, 2010;Karlsson et al, 2012;Prinz et al, 2013). The Ab 13-23 (HHQKLVFFAED) was synthesized and used in the thioflavin T test.…”

Section: Resultsmentioning

confidence: 99%