Novel asymmetric biscarbothioamides as Alzheimers disease associated cholinesterase inhibitors: synthesis, biological activity, and molecular docking studies
Yazarlar (7)
Halit Muğlu Kastamonu Üniversitesi, Türkiye
Doç. Dr. Hasan Yakan Ondokuz Mayıs Üniversitesi, Türkiye
Doç. Dr. Musa ERDOĞAN Kafkas Üniversitesi, Türkiye
Fevzi Topal Gümüşhane Üniversitesi, Türkiye
Prof. Dr. Meryem Topal Gümüşhane Üniversitesi, Türkiye
Prof. Dr. Cüneyt Türkeş Erzincan Binali Yıldırım Üniversitesi, Türkiye
Prof. Dr. Şükrü Beydemir Anadolu Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı New Journal of Chemistry (Q3)
Dergi ISSN 1144-0546 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 06-2024
Cilt / Sayı / Sayfa 48 / 24 / 10979–10989 DOI 10.1039/d4nj01462f
Makale Linki http://dx.doi.org/10.1039/d4nj01462f
UAK Araştırma Alanları
Organik Kimya
Özet
Exploring novel frameworks for treating Alzheimer's disease is an ambitious objective. In this particular context, a range of asymmetric biscarbothioamide derivatives (3a–l) with varying substitutions have been meticulously designed and effectively synthesized. The newly synthesized compounds have all been definitively characterized using established spectroscopic techniques such as 1H-NMR, 13C-NMR, FT-IR, and elemental analysis. In vitro, all the derivatives (3a–l) were evaluated to assess their inhibitory potential against cholinesterase enzymes (acetylcholinesterase, AChE, and butyrylcholinesterase, BChE). The outcomes demonstrated that these derivatives were potent and exhibited selectivity in inhibiting AChE, except for compounds 3b and 3e, which specifically inhibited BChE, showcasing varying degrees of KI values. Significantly, compounds 3j (KIs of 11.91 ± 2.25 nM for AChE and 77.76 ± 8.02 nM …
Anahtar Kelimeler