Home › Research › Treatments
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease
Simoni E, Daniele S, Bottegoni G, Pizzirani D, Trincavelli ML, Goldoni L, Tarozzo G, Reggiani A et al.. Journal of medicinal chemistry, 2012-10-17
Topic: Amyloid, tau and blood-test diagnosis
Herein we report on a novel series of multitargeted compounds obtained by linking together galantamine and memantine. The compounds were designed by taking advantage of the crystal structures of acetylcholinesterase (AChE) in complex with galantamine derivatives. Sixteen novel derivatives were synthesized, using spacers of different lengths and chemical composition. The molecules were then tested as inhibitors of AChE and as binders of the N-methyl-d-aspartate (NMDA) receptor (NMDAR). Some of the new compounds were nanomolar inhibitors of AChE and showed micromolar affinities for NMDAR. All compounds were also tested for selectivity toward NMDAR containing the 2B subunit (NR2B). Some of the new derivatives showed a micromolar affinity for NR2B. Finally, selected compounds were tested using a cell-based assay to measure their neuroprotective activity. Three of them showed a remarkable neuroprotective profile, inhibiting the NMDA-induced neurotoxicity at subnanomolar concentrations (e.g., 5, named memagal, IC(50) = 0.28 nM).
Cite this study APA, Vancouver, BibTeX · download .bib or .ris
APA 7th
Simoni, E., Daniele, S., Bottegoni, G., Pizzirani, D., Trincavelli, M. L., Goldoni, L., et al. (2012). Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease. Journal of medicinal chemistry. https://doi.org/10.1021/jm3009458
Vancouver
Simoni E, Daniele S, Bottegoni G, Pizzirani D, Trincavelli ML, Goldoni L, et al. Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease. Journal of medicinal chemistry. 2012. doi:10.1021/jm3009458. PMID: 23033965.
BibTeX
@article{simoni2012-23033965,
author = {Simoni, E. and Daniele, S. and Bottegoni, G. and Pizzirani, D. and Trincavelli, M. L. and Goldoni, L. and Tarozzo, G. and Reggiani, A. and others},
title = {{Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease}},
journal = {Journal of medicinal chemistry},
year = {2012},
doi = {10.1021/jm3009458},
pmid = {23033965},
url = {https://doi.org/10.1021/jm3009458}
}
Built from the record alzhub holds for this paper, not looked up. Volume, issue and page numbers are not held in the record. The record's author list ends in “et al.”, so not every author is named. Check the citation against the original before you use it.
Key findings
- Some of the new compounds were nanomolar inhibitors of AChE and showed micromolar affinities for NMDAR.
- All compounds were also tested for selectivity toward NMDAR containing the 2B subunit (NR2B).
- Some of the new derivatives showed a micromolar affinity for NR2B.
- Finally, selected compounds were tested using a cell-based assay to measure their neuroprotective activity.
- Three of them showed a remarkable neuroprotective profile, inhibiting the NMDA-induced neurotoxicity at subnanomolar concentrations (e.g., 5, named memagal, IC(50) = 0.28 nM).
New to this subject? Start with our plain-English guide: Treatments →
Study details
- Evidence strengthLow
How this study scored 36/100
Published in a peer-reviewed journal. Scored zero for study design, sample size, effect reported, studied in people and randomized / blinded because the record does not state it. We have no data on journal's citation record, times cited, citations per year, impact for its field and year, cited by studies here, still being cited, senior author's track record, institution's track record and multicenter collaboration, so those were left out: it earned 21 of the 58 points we could judge it on, which is 36 out of 100.
| Component | Points | Why |
|---|---|---|
| Journal tier | 7 / 10 | Tier 3 — peer-reviewed journal (Journal of medicinal chemistry) |
| Journal's citation record | — / 4 | No journal record from OpenAlex — left out of this score |
| Study design | 0 / 12 | No study design recorded — scores zero, not guessed (not stated in the record — scored 0) |
| Strength of evidence | 1 / 5 | Rated “low” in our summary |
| Peer-review validation | 10 / 10 | Peer-reviewed. Published as an article in a named peer-reviewed journal. |
| How recent | 1 / 5 | 2012 — within 20 year(s) of the newest study here |
| Sample size | 0 / 4 | Participant count not stated — scores zero (not stated in the record — scored 0) |
| Effect reported | 0 / 3 | No effect size reported — scores zero (not stated in the record — scored 0) |
| Studied in people | 0 / 3 | Not stated whether this was studied in people — scores zero (not stated in the record — scored 0) |
| Randomized / blinded | 0 / 2 | No randomization or blinding stated — scores zero (not stated in the record — scored 0) |
| Times cited | — / 7 | No citation count (not found in OpenAlex) — left out of this score |
| Citations per year | — / 5 | No citation count or no year — left out of this score |
| Impact for its field and year | — / 6 | No field-weighted citation impact (OpenAlex has none yet) — left out of this score |
| Cited by studies here | — / 6 | Not yet checked against this library's citation graph — left out of this score |
| Still being cited | — / 4 | No yearly citation counts — left out of this score |
| Senior author's track record | — / 4 | Senior author's record not available — left out of this score |
| Institution's track record | — / 3 | No institution listed in OpenAlex — left out of this score |
| Multicenter collaboration | — / 3 | Institutions not listed — left out of this score |
| Indexed in PubMed | 2 / 2 | Indexed in PubMed (PMID 23033965) |
| Free to read | 0 / 2 | Behind a paywall — scores zero |
| Points | 21 / 58 | Scored on 11 of 20 parts. We have no data for the rest, so they are left out: 21 of the 58 points we could judge it on is 36 out of 100. |
| Total | 36 / 100 | — |
What each of these 20 components measures, and what this score is not →
Read the original
Free copy unknown: no free-copy check has an answer for this record yet. That does not mean it is paywalled.
Related
Studies in the library that share something with this one. The line above each title says what.
Related studies in Treatments
Also tagged “memantine”
5 studies in the library carry the topic tag “memantine”; these are this study's neighbours in a fixed, alphabetical-by-hash tour of them, not the closest in content. All 5 tagged studies.