Synthesis, biological evaluation and molecular docking of novel 2-pyrazoline-1-carboxamides as anti-Alzheimer agents
Compounds <b>7</b> and <b>8</b> exhibited the best antioxidant activity. Compounds <b>7</b> and <b>8</b> were also the most potent compounds against AChE and BChE with IC<sub>50</sub> values of 2.77-3.09 µM and 6.16-6.79 µM, respectively, compared to galantamine (IC<sub>50</sub> = 1.90 µM for AChE and IC<sub>50</sub> = 46.51 µM for BChE). <i>In silico</i> studies showed that compound <b>7</b> binds to both targets with higher affinity than the reference compound, galantamine. ADME studies also showed that compound <b>7</b> can cross the blood-brain barrier.
Authors
- Sefer Baday (ORCID: https://orcid.org/0000-0002-2913-6687)
- Fatih Tok (ORCID: https://orcid.org/0000-0002-4569-008X)
- Zeynep Kuzu
- Fatma ÖZER (ORCID: https://orcid.org/0000-0002-6424-7235)
- Fethiye Aylin Sungur (ORCID: https://orcid.org/0000-0003-3245-742X)
- Yusuf Sıcak (ORCID: https://orcid.org/0000-0003-2339-5837)
- Mehmet Öztürk (ORCID: https://orcid.org/0000-0001-8932-4535)
- Fatih Kemaloğlu
Institutions
- Istanbul Technical University (TR)
- Marmara University (TR)
- Muğla University (TR)
Publication Details
- Journal
- Future Medicinal Chemistry
- Published
- 2025-12-01
- DOI
- https://doi.org/10.1080/17568919.2025.2594970
- Citations
- 1
- Primary Topic
- Chemical synthesis and alkaloids
- Type
- article
- Field-Weighted Citation Impact
- 0.94