1,2,3-Triazole Derivatives as Novel Antifibrinolytic Drugs
Abstract
:1. Introduction
2. Results
2.1. Synthesis
2.2. Clot Lysis Assays
2.3. Computational Analysis
3. Discussion
4. Materials and Methods
4.1. Synthesis
4.2. Clot Lysis Assay
4.3. Docking Studies
4.4. Molecular Dynamics Studies
4.5. Molecular Surface Determination
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
Abbreviations
References
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Compound | IC50 (µM) | Compound | IC50 (µM) |
---|---|---|---|
TXA | 33.3 | 6 | >1000 |
EACA | 263 | 7 | 335 |
1 | 13.8 | 8 | 27.8 |
2 | 138 | 9 | >1000 |
3 | >1000 | 10 | >1000 |
4 | >1000 | 11 | 60.4 |
5 | 36.8 |
Ligand | Molecular Surface (Å2) |
---|---|
GABA | 256.4 |
TXA | 293.7 |
4-PIOL | 310.9 |
1 | 374.4 |
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Bosch-Sanz, O.; Rabadà, Y.; Biarnés, X.; Pedreño, J.; Caveda, L.; Balcells, M.; Martorell, J.; Sánchez-García, D. 1,2,3-Triazole Derivatives as Novel Antifibrinolytic Drugs. Int. J. Mol. Sci. 2022, 23, 14942. https://doi.org/10.3390/ijms232314942
Bosch-Sanz O, Rabadà Y, Biarnés X, Pedreño J, Caveda L, Balcells M, Martorell J, Sánchez-García D. 1,2,3-Triazole Derivatives as Novel Antifibrinolytic Drugs. International Journal of Molecular Sciences. 2022; 23(23):14942. https://doi.org/10.3390/ijms232314942
Chicago/Turabian StyleBosch-Sanz, Oriol, Yvette Rabadà, Xevi Biarnés, Javier Pedreño, Luis Caveda, Mercedes Balcells, Jordi Martorell, and David Sánchez-García. 2022. "1,2,3-Triazole Derivatives as Novel Antifibrinolytic Drugs" International Journal of Molecular Sciences 23, no. 23: 14942. https://doi.org/10.3390/ijms232314942