New Thieno[3,2-d]Pyrimidin-4(3H)-One Schiff Bases as Selective Antileishmanial Agents
Yazarlar (4)
Prof. Dr. Neriman MOR Kafkas Üniversitesi, Türkiye
Dr. Öğr. Üyesi Barış Yıldız Kafkas Üniversitesi, Türkiye
Dr. Öğr. Üyesi Baycan MOR Kafkas Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | Life (Q1) | ||
| Dergi ISSN | 2075-1729 Dergi Bilgileri (2026) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 06-2026 |
| Cilt / Sayı / Sayfa | 16 / 6 / – | DOI | 10.3390/life16060979 |
| Makale Linki | https://doi.org/10.3390/life16060979 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| The present study aimed to design, synthesize, and evaluate a new series of thieno [3, 2-d] pyrimidin-4 (3H)-one-based Schiff bases as potential antileishmanial agents against Leishmania major (L. major). A series of twenty thieno [3, 2-d] pyrimidine Schiff base derivatives were synthesized and characterized using FTIR, NMR, and HRMS techniques. Their antipromastigote activities were evaluated in vitro against L. major, while cytotoxic effects were assessed on HUVECs to determine selectivity indices. The most active compound was further investigated using molecular docking against several L. major proteins. Among the tested compounds, compound 12, bearing a 2-hydroxy-5-bromophenyl moiety, exhibited the most potent activity against L. major promastigotes with an IC50 value of 13.7 µM, along with a favorable selectivity index (SI= 17.5), outperforming the reference drug miltefosine (IC50= 31 µM and SI … |
| Anahtar Kelimeler |
| antileishmania | L. major | leishmaniasis | Schiff bases | thieno[3,2-d]pyrimidin-4(3H)-one |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Google Scholar | 1 |