Synthesis of new carboxylates and sulfonates containing thiazolidin-4-one ring and evaluation of inhibitory properties against some metabolic enzymes
Yazarlar (6)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Doç. Dr. Parham Taslımı Bartın Üniversitesi, Türkiye
Prof. Dr. Burak Tüzün Sivas Cumhuriyet Üniversitesi, Türkiye
Dr. Öğr. Üyesi Ahmet Karakuş Bartin Üniversitesi, Türkiye
Dr. Öğr. Üyesi Nastaran Sadeghıan Bartın Üniversitesi, Türkiye
Prof. Dr. İlhami Gülçin Atatürk Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Journal of the Iranian Chemical Society (Q3) | ||
| Dergi ISSN | 1735-207X Dergi Bilgileri (2023) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 10-2023 |
| Cilt / Sayı / Sayfa | 20 / 10 / 2631–2642 | DOI | 10.1007/s13738-023-02861-3 |
| Makale Linki | http://dx.doi.org/10.1007/s13738-023-02861-3 | ||
| UAK Araştırma Alanları |
Organik Kimya
Spektroskopi
Biyokimya
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| Özet |
| A series of thizaolidin-4-one derivatives (3a-o) was synthesized with excellent yield (94–97%) and the structures of the compounds were characterized with Fourier-transform Infrared (FTIR), Nuclear Magnetic Resonance (1H NMR—13C NMR), and High-resolution Mass Spectroscopy (HRMS). Novel compounds were tested towards some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I-II (hCA I-II). All the synthetic analogs had potent inhibitory strength with Ki values in the range of 161.28 ± 16.91–943.13 ± 57.23nM against hCA-I and 151.77 ± 21.42–879.89 ± 57.70 nM against hCA-II in comparison to the standard acetazolamide Ki = 847.18 ± 75.41nM (for hCA-I) and Ki = 776.12 ± 70.62nM (for hCA-II). Most of the compounds showed potent inhibitory activity against AChE and BChE enzymes with IC50 value 823.71–984 … |
| Anahtar Kelimeler |
| ADME/T | Enzyme inhibition | Molecular docking | Synthesis | Thizaolidin-4-one |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 39 |
| Scopus | 38 |
| Google Scholar | 45 |