Synthesis, Neuroprotective Effect and Physicochemical Studies of Novel Peptide and Nootropic Analogues of Alzheimer Disease Drug
Abstract
:1. Introduction
2. Results and Discussion
2.1. Chemistry
2.2. Novel Structural Derivatives of Memantine Improve Cell Viability against Copper-Induced Neurotoxicity in APPswe Cells
2.3. Novel Structural Derivatives of Memantine Improve Cell Viability against Glutamate-Induced Neurotoxicity in SH-SY5Y Cells
2.4. Prediction of EC50 Using HYBOT Descriptors
2.5. Solubility Experiments
3. Materials and Methods
3.1. Materials
3.1.1. Chemicals
3.1.2. Solvents
3.1.3. Cell Culture and Treatment
3.2. Chemical Synthesis
3.3. Measurement of Neuroprotective Effects against Copper-Induced Toxicity in APPswe Cells
3.4. Measurement of Neuroprotective Effects against Glutamate-Induced Toxicity in SH-SY5Y Cells
3.5. Cell Viability Assay
3.6. Statistical Analysis
3.7. Solubility Determination
3.8. Powder X-ray Diffraction (PXRD) Were Recorded According to SUROV et al. [37]
3.9. QSAR Modelling and Calculation of HYBOT Descriptors
4. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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№ Compound | pH 2.0 | pH 7.4 |
---|---|---|
S2·103 (M) | S2·104 (M) | |
(1) | 0.873 ± 0.022 | 9.93 ± 0.25 |
(2) | 1.25 ± 0.03 | 2.10 ± 0.05 |
(3) | 1.02 ± 0.03 | 1.15 ± 0.03 |
(4) | 0.321 ± 0.008 | 3.44 ± 0.09 |
(5) | 6.67 ± 0.17 | 71.5 ± 1.8 |
(6) | 25.88 ± 0.65 | 201.8 ± 5.1 |
(8) a | 205.1 ± 5.1 | 269.2 ± 6.7 |
(9) a | 75.9 ± 1.9 | 136.1 ± 3.4 |
(10) a | 46.2 ± 1.1 | 83.0 ± 2.1 |
(11) a | 118.0 ± 3.0 | 804 ± 20 |
(12) a | 175.0 ± 4.4 | 164.1 ± 4.1 |
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Chayrov, R.; Volkova, T.; Perlovich, G.; Zeng, L.; Li, Z.; Štícha, M.; Liu, R.; Stankova, I. Synthesis, Neuroprotective Effect and Physicochemical Studies of Novel Peptide and Nootropic Analogues of Alzheimer Disease Drug. Pharmaceuticals 2022, 15, 1108. https://doi.org/10.3390/ph15091108
Chayrov R, Volkova T, Perlovich G, Zeng L, Li Z, Štícha M, Liu R, Stankova I. Synthesis, Neuroprotective Effect and Physicochemical Studies of Novel Peptide and Nootropic Analogues of Alzheimer Disease Drug. Pharmaceuticals. 2022; 15(9):1108. https://doi.org/10.3390/ph15091108
Chicago/Turabian StyleChayrov, Radoslav, Tatyana Volkova, German Perlovich, Li Zeng, Zhuorong Li, Martin Štícha, Rui Liu, and Ivanka Stankova. 2022. "Synthesis, Neuroprotective Effect and Physicochemical Studies of Novel Peptide and Nootropic Analogues of Alzheimer Disease Drug" Pharmaceuticals 15, no. 9: 1108. https://doi.org/10.3390/ph15091108