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Record W4200153774 · doi:10.3390/ecmc2021-11537

Novel selenium-based molecules as drug candidates for Alzheimer`s disease

2021· article· en· W4200153774 on OpenAlexaff
Ahmed A. Hefny, Praveen P. N. Rao

Bibliographic record

VenueProceedings of 7th International Electronic Conference on Medicinal Chemistry · 2021
Typearticle
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicOrganoselenium and organotellurium chemistry
Canadian institutionsUniversity of Waterloo
Fundersnot available
KeywordsSeleniumDrugDiseaseComputer scienceAlzheimer's diseaseDrug discoveryMedicinePharmacologyChemistryPathologyBiochemistry

Abstract

fetched live from OpenAlex

Although Alzheimer’s disease (AD) was first diagnosed over 100 years ago, the number of therapeutic options remains very limited, and the drug discovery process for AD is painstakingly slow. This is attributed to the complexity of the disease's pathophysiology. Consequently, AD research has shifted from a monotherapy approach into a multi-targeted approach where one molecule is able to hit multiple targets. Organoselenium compounds as multi-targeted drug ligands (MTDLs) have been developed as potential inhibitors of Aβ aggregation and to reduce oxidative stress in AD, and also to provide novel scaffolds for designing promising disease-modifying agents. By utilizing computational chemistry principles, organoselenium tricyclic scaffolds were designed that exhibited promising binding affinity, and efficiency toward Aβ protein, different organic chemistry procedures were applied to develop synthetic methods to obtain the target derivatives. Further studies include structure-activity relationship (SAR) optimization by carrying out in vitro fluorescence kinetic studies to determine the inhibition of Aβ40 aggregation, transmission electron microscopy (TEM) studies, evaluation of antioxidant properties, and cell culture studies to identify novel organoselenium derivatives as MTDLs. Preliminary studies demonstrate a significant reduction in the Aβ40 aggregation suggesting their application in the development of novel therapeutic agents for the treatment of AD.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.003
Threshold uncertainty score0.010

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0030.001

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.047
GPT teacher head0.377
Teacher spread0.329 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations0
Published2021
Admission routes1
Has abstractyes

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Same venueProceedings of 7th International Electronic Conference on Medicinal ChemistrySame topicOrganoselenium and organotellurium chemistryFrench-language works237,207