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Novel styryl-thiazo...
Novel styryl-thiazole hybrids as potential anti-Alzheimer's agents
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- Gouleni, Niki (författare)
- Natl & Kapodistrian Univ Athens, Dept Chem, Organ Chem Lab, Athens, Greece.
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- Di Rienzo, Annalisa (författare)
- G DAnnunzio Univ Chieti Pescara, Dept Pharm, I-66100 Chieti, CH, Italy.
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- Yilmaz, Ahmet (författare)
- Erzurum Tech Univ, Dept Mol Biol & Genet, Fac Sci, TR-25050 Erzurum, Turkiye.
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- Selvitopi, Harun (författare)
- Erzurum Tech Univ, Dept Math, Fac Sci, TR-25050 Erzurum, Turkiye.
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- Arslan, Mehmet Enes (författare)
- Erzurum Tech Univ, Dept Mol Biol & Genet, Fac Sci, TR-25050 Erzurum, Turkiye.
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- Mardinoglu, Adil (författare)
- KTH,Systembiologi,Science for Life Laboratory, SciLifeLab,Kings Coll London, Ctr Host Microbiome Interact, Fac Dent Oral & Craniofacial Sci, London SE1 9RT, England.
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- Turkez, Hasan (författare)
- Ataturk Univ, Dept Med Biol, Fac Med, Erzurum, Turkiye.
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- Di Stefano, Antonio (författare)
- G DAnnunzio Univ Chieti Pescara, Dept Pharm, I-66100 Chieti, CH, Italy.
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- Vassiliou, Stamatia (författare)
- Natl & Kapodistrian Univ Athens, Dept Chem, Organ Chem Lab, Athens, Greece.
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- Cacciatore, Ivana (författare)
- G DAnnunzio Univ Chieti Pescara, Dept Pharm, I-66100 Chieti, CH, Italy.
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Natl & Kapodistrian Univ Athens, Dept Chem, Organ Chem Lab, Athens, Greece G DAnnunzio Univ Chieti Pescara, Dept Pharm, I-66100 Chieti, CH, Italy. (creator_code:org_t)
- Royal Society of Chemistry (RSC), 2023
- 2023
- Engelska.
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Ingår i: RSC Medicinal Chemistry. - : Royal Society of Chemistry (RSC). - 2632-8682. ; 14:11, s. 2315-2326
- Relaterad länk:
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https://doi.org/10.1...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- In this study, combining the thiazole and cinnamoyl groups into the styryl-thiazole scaffold, a series of novel styryl-thiazole hybrids (6a-p) was rationally designed, synthesized, and evaluated by the multi-target-directed ligands strategy as potential candidates for the treatment of Alzheimer's disease (AD). Hybrids 6e and 6i are the most promising among the synthesized hybrids since they are able to significantly increase cell viabilities in A beta 1-42-exposed-human neuroblastoma cell line (6i at the concentration of 50 mu g mL-1 and 6e at the concentration of 25 mu g mL-1 resulted in similar to 34% and similar to 30% increase in cell viabilities, respectively). Compounds 6e and 6i exhibit highly AChE inhibitory properties in the experimental AD model at 375.6 +/- 18.425 mU mL-1 and 397.6 +/- 32.152 mU mL-1, respectively. Moreover, these data were also confirmed by docking studies and in vitro enzyme inhibition assays. Compared to hybrid 6e and according to the results, 6i also has the highest potential against A beta 1-42 aggregation with over 80% preventive activity. The in silico prediction of the physicochemical properties confirms that 6i possesses a better profile compared to 6e. Therefore, compound 6i presents a promising multi-targeted active molecular profile for treating AD considering the multifactorial nature of AD, and it is reasonable to deepen its mechanisms of action in an in vivo experimental model of AD. Novel styryl-thiazole hybrids (6a-p) was rationally designed, synthesized, and evaluated by the multi-target-directed ligands strategy as potential candidates for the treatment of Alzheimer's disease.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Neurovetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Neurosciences (hsv//eng)
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- Av författaren/redakt...
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Gouleni, Niki
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Di Rienzo, Annal ...
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Yilmaz, Ahmet
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Selvitopi, Harun
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Arslan, Mehmet E ...
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Mardinoglu, Adil
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visa fler...
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Turkez, Hasan
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Di Stefano, Anto ...
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Vassiliou, Stama ...
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Cacciatore, Ivan ...
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visa färre...
- Om ämnet
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- MEDICIN OCH HÄLSOVETENSKAP
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MEDICIN OCH HÄLS ...
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och Medicinska och f ...
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och Neurovetenskaper
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RSC Medicinal Ch ...
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