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Record W3146190083 · doi:10.21203/rs.3.rs-223104/v1

Synthesis, characterization and antimicrobial properties of two derivatives of pyrrolidine-2,5-dione fused at positions-3,4 to a dibenzobarrelene backbone

2021· preprint· en· W3146190083 on OpenAlexaff
Emmanuel Sopbué Fondjo, Abdou Salamou Njoya, Jean‐de‐Dieu Tamokou, Giscard Doungmo, Bruno Lenta Djakou, Peter F. W. Simon, Appolinaire Tsopmo, Jules‐Roger Kuiate

Bibliographic record

VenueResearch Square · 2021
Typepreprint
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicBioactive Compounds and Antitumor Agents
Canadian institutionsCarleton University
FundersDeutscher Akademischer Austauschdienst
KeywordsChemistryAntimicrobialPyrrolidineAnilineStereochemistryProton NMRChemical structureCombinatorial chemistryOrganic chemistry

Abstract

fetched live from OpenAlex

Abstract Background : The present study describes for the first time, the synthesis of two pyrrolidine-2,5-dione derivatives that belong to N-arylsuccinimid (compound 5 ) and of azo (compound 8 ) class of molecules. The initial step of the reaction involved the preparation of the intermediate compound (9R, 10R, 11S)-9, 10-dihydro-9, 10-[3, 4] furanoanthracene-12, 14-dione ( 3 ) through [4 + 2]-cycloaddition between anthracene and maleic anhydride in xylene which was then condensed with para- hydroxyaniline to give compound 5 . Subsequent coupling of 5 with the aryldiazonium ion of aniline gave compound 8 . Results : These compounds were characterized by their physical, elemental, and spectroscopic data. 2D-NMR (COSY, HSQC, and HMBC) techniques were used to complete the elucidation of their structures. Compounds 5 (MIC = 32–128µg/mL) and 8 (MIC = 16–256µg/mL) along with the precursor 3 (MIC = 64–128µg/mL) displayed moderate antimicrobial activities against selected bacterial and fungal species when compared with those of nystatin (MIC = 0.50–2µg/mL) and ciprofloxacin (MIC = 0.50–16µg/mL) used as reference drugs. Conclusion : The results of biological tests showed that compounds 3 , 5 , 8 possess antimicrobial activities. Although being less active than the compound taken as a reference, the azo compound has better antibacterial activity than the other two compounds especially on Staphylococcus aureus , V. cholerae SG24 and, V. cholerae CO6 strains. These results show that the azo function (N = N) is indeed a pharmacophore and would be responsible for the biological activity in the azo molecules.

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 distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.001
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow)
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 score0.028
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0000.000
Science and technology studies0.0000.001
Scholarly communication0.0000.000
Open science0.0000.002
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0000.000

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 head0.219
GPT teacher head0.467
Teacher spread0.248 · 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 teacher head, not a consensus.

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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