1‐[(Imidazolidin‐2‐yl)imino]‐1<i>H</i>‐indoles as new hypotensive agents: synthesis and<i>in vitro</i>and<i>in vivo</i>biological studies
Bibliographic record
Abstract
A series of 1‐[(imidazolidin‐2‐yl)imino]‐1 H ‐indole analogues of hypotensive α 2 ‐AR agonists, 1‐[(imidazolidin‐2‐yl)imino]‐1 H ‐indazoles, was synthesized and tested in vitro for their activities at α 1 ‐ and α 2 ‐adrenoceptors as well as imidazoline I 1 and I 2 receptors. The most active 1‐[(imidazolidin‐2‐yl)imino]‐1 H ‐indoles displayed high or moderate affinities for α 1 ‐ and α 2 ‐adrenoceptors and substantial selectivity for α 2 ‐adrenoceptors over imidazoline‐I 1 binding sites. The in vivo cardiovascular properties of indole derivatives 3 revealed that substitution at C‐7 position of the indole ring may result in compounds with high cardiovascular activity. Among them, 7‐fluoro congener 3g showed the most pronounced hypotensive and bradycardic activities in this experiment at a dose as low as 10 μg/kg i.v. Metabolic stability of the selected compounds of type 3 was determined using both in vitro and in silico approaches. The results indicated that these compounds are not vulnerable to rapid first‐phase oxidative metabolism.
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How this classification was reachedexpand
Full frame distilled prediction
Teacher imitationNot 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.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.006 |
| Meta-epidemiology (narrow) | 0.001 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.001 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.001 | 0.000 |
| Insufficient payload (model declined to judge) | 0.000 | 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 teacher head, 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".