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Dergiler / Cumhuriyet Science Journal / 2022 / Cilt: 43 - Sayı: 4

Acetylcholinesterase Inhibitor Activity of Some 5-Nitrothiophene-Thiazole Derivatives

Demokrat NUHA
Asaf Evrim EVREN
Zennure Şevval ÇİYANCI
Halide Edip TEMEL
Gülşen AKALIN ÇİFTÇİ
Leyla YURTTAŞ
Sayfa
584–589
Yayın Tarihi
2022-12-27
DOI
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⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

It was determined that the compounds exhibited inhibition of between 33.66–47.96 % against AChE and 13.03–63.29 % against BuChE at 80 µg/mL concentration.

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Amaç & Hipotez:The potential anticholinesterase characteristics of some thiazole derivatives (2a–2j), including the 5-nitrothiophene moiety, were examined in this work. 1H-NMR, 13C-NMR, and HRMS spectral data were used to determine the structure of the compounds.
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Temel Bulgular & Veri:Using a modified Ellman's spectrophotometric approach, each compound was tested for its ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes.
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Sonuç & Katkı:It was determined that the compounds exhibited inhibition of between 33.66–47.96 % against AChE and 13.03–63.29 % against BuChE at 80 µg/mL concentration.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:PET-RAFT polymerization · Grafting from method · Bioconjugation

Abstract

The potential anticholinesterase characteristics of some thiazole derivatives (2a–2j), including the 5-nitrothiophene moiety, were examined in this work. 1H-NMR, 13C-NMR, and HRMS spectral data were used to determine the structure of the compounds. Using a modified Ellman's spectrophotometric approach, each compound was tested for its ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. It was determined that the compounds exhibited inhibition of between 33.66–47.96 % against AChE and 13.03–63.29 % against BuChE at 80 µg/mL concentration.

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Bu Makaleye Atıf Yap

NUHA, D., EVREN, A. E., ÇİYANCI, Z. Ş., TEMEL, H. E., ÇİFTÇİ, G. A., YURTTAŞ, L. (2022). Acetylcholinesterase Inhibitor Activity of Some 5-Nitrothiophene-Thiazole Derivatives. Cumhuriyet Science Journal, Cilt: 43 - Sayı: 4, 584–589. https://ajindex.com/articles/885446

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Kaynakça (11)

  1. Vaz M., Silvestre S., Alzheimer's disease: Recent treatment strategies, Eur. J. Pharmacol, 887 (2020) 173554
  2. Bateman R.M., Glacial progress: do we finally understand the narrow-leaved marsh-orchids?, New Journal of Botany, 1(1) (2013) 2-15
  3. Zhou B., Li D., Cui J., Li D., Geng H., Gao J., Zhou B., Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase, European Journal of Medicinal Chemistry, 200 (2020) 1-11
  4. Zhao S., Xu J., Zhang H., Han C.K., Wu J., Li D., Hu C.J. (2021). Multivalent butyrylcholinesterase inhibitor discovered by exploiting dynamic combinatorial chemistry. Bioorganic Chemistry, 108, 104656
  5. Sun J., Wang H., Lei Z., Yue S., Chen J., Sun J., Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors, European Journal of Medicinal Chemistry, 234 (2022) 114210
  6. Mao F., Wang H., Ni W., Zheng X., Wang M., Bao K., Ling D., Li X., Xu Y., Zhang H., Design, synthesis, and biological evaluation of orally available first-generation dual-target selective inhibitors of acetylcholinesterase (AChE) and phosphodiesterase 5 (PDE5) for the treatment of Alzheimer’s disease, ACS Chemical Neuroscience, 9(2) (2018) 328-345
  7. Kurt B.Z., Gazioglu I., Basile L., Sonmez F., Ginex T., Kucukislamoglu M., Guccione S., Potential of aryl–urea–benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease, European Journal of Medicinal Chemistry, 102 (2015) 80-92
  8. Romero A., Cacabelos R., Oset-Gasque M.J., Samadi A., Marco-Contelles J., Novel tacrine-related drugs as potential candidates for the treatment of Alzheimer’s disease, Bioorganic & Medicinal Chemistry Letters, 23(7) (2013) 1916-1922
  9. Kandiah N., Pai M.-C., Senanarong V., Looi I., Ampil E., Park K.W., Karanam A.K., Christopher S., Rivastigmine: the advantages of dual inhibition of acetylcholinesterase and butyrylcholinesterase and its role in subcortical vascular dementia and Parkinson’s disease dementia, Clinical Interventions in Aging, 12 (2017) 697
  10. Evren A.E., Nuha D., Dawbaa S., Saglik B.N., Yurttas L., Synthesis of novel thiazolyl hydrazone derivatives as potent dual monoamine oxidase-aromatase inhibitors, Eur. J. Med. Chem., 229 (2022) 114097
  11. Sabry M.A., Ghaly M.A., Maarouf A.R., El-Subbagh H.I., New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Syn