Derivatives of 2-Aminopyridines as Inhibitors of Multidrug Resistant Staphylococcus Aureus Strains
Bibliographic record
Abstract
A new series of 2-aminopyridine derivatives were synthesised. N-acylation of 2-amino-3-chloro-5-(trifluoromethyl) pyridine and 2-amino-5-(trifluoromethyl) pyridine with series of acid chlorides afforded a total of fourteen (14) amide compounds. The structures of the new compounds have been established by their IR, NMR and mass spectra data. All the compounds were tested for their activity against four (4) multi-drug resistant (MDR) bacteria Staphylococcus aureus strains using microplate alamar blue assay. The MDR-Staphylococcus aureus strains employed for this study were Epidermic Methicilin Resistant Staphylococcus aureus (EMRSA-17), Methicilin Resistant Staphylococcus aureus (MRSA-252), Epidermic Methicilin Resistant Staphylococcus aureus (EMRSA-16) and Pakistani Drug resistant clinical isolate of Staphylococcus aureus (PRSA). Other bacteria strains also used include Escherichia coli (ATCC 2592), Shigella flexenari (ATCC 12022), Staphylococcus aureus (NCTC 6571) and Pseudomonas aeruginosa (NCTC 10662). The synthesised compounds exhibited very good activity against the four MDR-Staphylococcus aureus strains of which most of the compounds showed higher potencies for inhibiting the growth of the strains than vancomycin, the standard drug employed. The compounds reported here may serve as the starting point for the design and development of MDR-S.aureus inhibitors as antibacterial agents.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot 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.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.001 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.001 |
| Insufficient payload (model declined to judge) | 0.002 | 0.000 |
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.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
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".