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Record W2524406518 · doi:10.1002/slct.201600789

Antimicrobial and Antitumor Screening of Fluorescent 5,7‐Dihydroxy‐4‐Propyl‐ <i>2H</i> ‐Chromen‐2‐One Derivatives with Docking Studies

2016· article· en· W2524406518 on OpenAlexafffund
Alaa S. Abd‐El‐Aziz, Azhaar T. Alsaggaf, Rawda M. Okasha, Hany E. A. Ahmed, Rabin Bissessur, Amani A. Abdelghani, Tarek H. Afifi

Bibliographic record

VenueChemistrySelect · 2016
Typearticle
Languageen
FieldChemistry
TopicSynthesis and biological activity
Canadian institutionsUniversity of Prince Edward Island
FundersNatural Sciences and Engineering Research Council of CanadaMinistry of Education, IndiaTaibah UniversityMinistry of Earth Sciences
KeywordsAntimicrobialDNA gyraseNovobiocinDocking (animal)ChemistryStereochemistryFluorescenceCombinatorial chemistryPotencyBiochemistryAntibioticsIn vitroEscherichia coliOrganic chemistry

Abstract

fetched live from OpenAlex

Abstract A series of novel fluorescent 5,7‐dihydroxy‐4‐propyl‐2 H ‐chromen‐2‐one derivatives ( 2a–j ) were synthesized and were found to absorb around 322 and 410 nm.All compounds except the nitro‐containing compound exhibited emission wavelengths around 450 nm with good fluorescence quantum yields ( Φ F ). Their antimicrobial activity was investigated and tested against several human pathogen Gram‐positive, Gram‐negative bacteria and fungi as well as mycobacterium using agar well diffusion method and minimum inhibitory concentrations were reported. All compounds showed significantly potent antimicrobial activities against most bacterial strains compared to reference drugs. Due to their structural similarity to reference drugs clorobiocin and novobiocin, the docking experiments in the ATP binding pocket of DNA gyrase B enzyme revealed that the compounds mostly have the same binding mode as the reference drugs. Moreover, the cytotoxic activity was also evaluated against four different human cell lines and exhibited more potency than the reference drug.

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 score0.001
Threshold uncertainty score0.004

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)0.0010.000

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 head0.035
GPT teacher head0.246
Teacher spread0.211 · 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

Citations19
Published2016
Admission routes2
Has abstractyes

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