New biocidal hybrids bearing acridine and aminophosphonate Scaffolds against different bacterial pathogens
Bibliographic record
Abstract
New hybrids containing acridine and α-amino phosphonate scaffolds 6a-h were synthesized by three one-pot reactions via Kabachnik–Fields reaction of 9-aminoacridine derivatives 3a-d, aldehydes 4a,b and triphenyl phosphite 5 in equimolar ratio under stirring at room temperature. The installation of the afforded hybrids was affirmed by different spectroscopic methods as IR, 1HNMR, 13CNMR, 31P NMR, MS and elemental analysis. The antibacterial activities of hybrids 6a-h were screened against both Gram-positive and Gram-negative bacteria of four pathogenic strains, comparable to ampicillin and chloramphenicol drugs. Most hybrids showed higher activity compared to the reference drugs. Notably, the antibacterial performance of 6c was more substantial than other analogues with best minimum inhibitory concentration (MIC) and highest zone of inhibition (ZOI) of 31, 34, 35, 38 mm, against Serratia marcescens, Streptococcus mutans, MRSA and Klebsiella pneumoniae clinical isolates respectively. In addition, Transmission Electron Microscopes (TEM) was carried out to study the mode of action of 6c with MRSA, the results confirmed that the titled hybrid caused the disruption of bacterial cell wall. Moreover, the time-dependent kill study revealed that the investigated compounds were time and dose-effective bactericidal agents and could be used as potential leads for further development and optimization of novel 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 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 0.001 |
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.
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".