Synthesis of 5-aryl/heterylidene substituted 2-imino-4-thiazolidinones possessing 1,3,4-thiadiazole moiety and their antitrypanosomal activity
Bibliographic record
Abstract
A novel 1,3,4-thiadiazole containing 2-iminothiazolidine-4-ones 4a-b were synthesized through the reaction of 2-chloro-N-(5-ethyl/allylsulfanyl-[1,3,4]thiadiazol-2-yl)-acetamides 1a-b with ammonium thiocyanate in dry acetone. Condensation of 4a-b with various carbonyl compounds according to the standard Knoevenagel procedure yielded the corresponding 5-arylidene- (5a-d), 5-heterylidene- (6a-c), 5-isatinylidene- (7a-b) and 5-(3-phenyl-2-propene-1-ylidene)- (8a-b) derivatives. All the newly synthesized compounds were confirmed by their elemental analysis and spectral data. Synthesized compounds 4a, 5a, 5b, 6a, 6c and 7a were screened for their in vitro antitrypanosomal activity against T. brucei gambience (Feo strain). The 5-ylidene substituted compounds with S-allyl group in position 5 of thiadiazole cycle (5a, 5b, 6a and 7a) displayed good to excellent antitrypanosomal potency with a range IC50 = 7.3-12.8 µM.
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 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 | 0.001 |
| Meta-epidemiology (narrow) | 0.000 | 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 | 0.000 | 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".