Design, synthesis, and multitarget evaluation of thiosemicarbazone–sulfonamide hybrids as potent cholinesterase and MAO-A inhibitors with neuroblastoma-associated cytotoxicity
Yazarlar (11)
Khawar Abbas
Bahauddin Zakariya University, Pakistan
Bahauddin Zakariya University, Pakistan
Mohamed Rahmtalla Elamın Imam Mohammad Ibn Saud Islamic University, Suudi Arabistan
Doç. Dr. HALİL Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Arş. Gör. Furkan Çakır Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Doç. Dr. Parham Taslımı Bartın Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Nadeem Raza
Imam Mohammad Ibn Saud Islamic University, Suudi Arabistan
Imam Mohammad Ibn Saud Islamic University, Suudi Arabistan
Mostafa E. Salem
Imam Mohammad Ibn Saud Islamic University, Suudi Arabistan
Imam Mohammad Ibn Saud Islamic University, Suudi Arabistan
Rıma D. Alharthy King Abdulaziz University, Suudi Arabistan
Asıf Rasool Nanjing University, Çin
Zahıd Shafıq Bahauddin Zakariya University, Pakistan
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | Scientific Reports (Q1) | ||
| Dergi ISSN | 2045-2322 Dergi Bilgileri (2026) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 05-2026 |
| Cilt / Sayı / Sayfa | 16 / 1 / – | DOI | 10.1038/s41598-026-52909-6 |
| Makale Linki | https://doi.org/10.1038/s41598-026-52909-6 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| Neurodegenerative disorders and neuroblastoma represent major therapeutic challenges, and multitarget approaches have gained increasing attention. In this study, a series of thiosemicarbazone derivatives (5a–t) was evaluated for their inhibitory activity against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and monoamine oxidase A (MAO-A), together with their cytotoxic effects and molecular interaction profiles. In vitro enzyme assays revealed nanomolar inhibition for several compounds. Notably, compound 5n exhibited potent and balanced multitarget activity with IC50 values of 104.28 nM (AChE), 23.04 nM (BChE), and 215.50 nM (MAO-A), surpassing galantamine (IC50 = 296.32 and 105.20 nM for AChE and BChE, respectively) and approaching the activity of clorgyline (IC50 = 401.68 nM). Kinetic studies confirmed strong enzyme binding, with Ki values of 92.42 nM (AChE) and 25.35 nM … |
| Anahtar Kelimeler |
| Cholinesterase | Monoamine oxidase A | Neuroblastoma | Neurodegenerative disorders | Thiosemicarbazone |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 1 |
| Scopus | 1 |
| Google Scholar | 1 |