The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Inhibition of Monoamine Oxidases by Functionalized Coumarin Derivatives: Biological Activities, QSARs, and 3D-QSARs
Open accessAbstract
A large series of coumarin derivatives (71 compounds) were tested for their monoamine oxidase A and B (MAO-A and MAO-B) inhibitory activity. Most of the compounds acted preferentially on MAO-B with IC(50) values in the micromolar to low-nanomolar range; high inhibitory activities toward MAO-A were also measured for sulfonic acid esters. The most active compound was 7-[(3, 4-difluorobenzyl)oxy]-3,4-dimethylcoumarin, with an IC(50) value toward MAO-B of 1.14 nM. A QSAR study of 7-X-benzyloxy meta-substituted 3,4-dimethylcoumarin derivatives acting on MAO-B yielded good statistical results (q(2)() = 0.72, r(2)() = 0.86), revealing the importance of lipophilic interactions in modulating the inhibition and excluding any dependence on electronic properties. CoMFA was performed on two data sets of MAO-A and MAO-B inhibitors. The GOLPE procedure, with variable selection criteria, was applied to improve the predictivity of the models and to facilitate the graphical interpretation of results.
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Cramer, R. D., Patterson, D. E., & Bunce, J. D. (1988) · Journal of the American Chemical Society · doi:10.1021/ja00226a005 · Cited by 3,931
Cited by
Multi-target-Directed Ligands To Combat Neurodegenerative Diseases
Cavalli, A., Bolognesi, M. L., Minarini, A., Rosini, M., Tumiatti, V., Recanatini, M., & Melchiorre, C. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm7009364 · Cited by 1,152
Binda, C., Wang, J., Pisani, L., Caccia, C., Carotti, A., Salvati, P., Edmondson, D. E., & Mattevi, A. (2007) · Journal of Medicinal Chemistry · doi:10.1021/jm070677y · Cited by 607
Self-citationTopological Polar Surface Area: A Useful Descriptor in 2D-QSAR
Prasanna, S., & Doerksen, R. (2009) · Current Medicinal Chemistry · doi:10.2174/092986709787002817 · Cited by 484
Coumarins Derivatives as Dual Inhibitors of Acetylcholinesterase and Monoamine Oxidase
Brühlmann, C., Ooms, F., Carrupt, P.-A., Testa, B., Catto, M., Leonetti, F., Altomare, C., & Carotti, A. (2001) · Journal of Medicinal Chemistry · doi:10.1021/jm010894d · Cited by 290
Self-citationLi, X., Li, T., Zhan, F., Cheng, F., Lu, L., Zhang, B., Li, J., Hu, Z., Zhou, S., Jia, Y., et al. (2022) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.2c00520 · Cited by 18
Metadata
- Authors
- Gnerre, C., Catto, M., Leonetti, F., Weber, P., Carrupt, P.-A., Altomare, C., Carotti, A., & Testa, B.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2000-11-11
- Volume
- 43
- Issue
- 25
- Pages
- 4747-4758
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1971019239
- Cited by
- 262
- References
- 1
- FWCI
- 9.00
- Type
- journal article
- Language
- en
- Open access
- green
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