Pharmacokinetic study of two sulfamethoxazole-phytochemical antimicrobial conjugates in mice
Bibliographic record
Abstract
Antimicrobial resistance (AMR) has emerged to be a big threat to both human and animal health. Along the tighter control on antibiotic use, developing novel therapeutic agents and approaches is crucial for combating AMR. We recently designed and synthesized several antibiotic-phytochemical conjugates which exhibited potent antimicrobial activities. To understand their pharmacological behavior and obtain a guideline for further drug development, we undertook a pharmacokinetic study on sulfamethoxazole-gallate and sulfamethoxazole-caffeate. Cmax was determined to be 842 ± 544 ng/mL at dose of 1500 mg/kg and 733 ± 477 ng/mL at dose of 2000 mg/kg for sulfamethoxazole-gallate and 211 ± 100 at a dose of 150 mg/kg and 755 ± 705 ng/mL at dose of 300 mg/kg for sulfamethoxazole-caffeate. Tmax was 1 h for sulfamethoxazole-gallate under both doses and 0.5 h for sulfamethoxazole-caffeate under both doses. Since Cmax was significantly lower than the in vitro MIC for both conjugates, more formulations and administration routes such as IV injection will be investigated in our future studies.
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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) | 0.001 | 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".