A potential insect growth regulator for cockroach control: design, synthesis and bioactivity of N‐terminal‐modified allatostatin analogues
Bibliographic record
Abstract
Abstract BACKGROUND The FGLa ‐allatostatins ( ASTs ) are a family of neuropeptides that can inhibit juvenile hormone biosynthesis by the corpora allata ( CA ) in vitro , and therefore they are regarded as insect growth regulator ( IGR ) candidates for pest control. In our previous studies, an AST mimic, H17 , was found to have a significant effect on JH biosynthesis by cockroach CA , both in vitro and in vivo . To discover new potential mimics and explore the substituent effect on the inhibition of JH biosynthesis, 30 analogues, modified with various substituents on the benzene ring at the N‐terminus of lead compound H17 , were designed and synthesised. Their bioactivity in inhibiting JH biosynthesis by the CA of Diploptera punctata and the potency of M9 , M10 and M11 in activation of Dippu‐ AstR were evaluated. RESULTS All the analogues showed an effect on JH biosynthesis by CA in vitro . M9 , M10 and M11 can activate the Dippu‐ AstR , albeit with much lower potency than that of AST 1. M11 also exhibited improved in vitro activity ( IC 50 6.98 n m ) in comparison with the lead compound H17 ( IC 50 29.5 n m ). In particular, M11 displayed good in vivo activity in inhibiting JH biosynthesis and basal oocyte growth. CONCLUSION The structure–activity relationship studies suggest that different positions of substituents on the benzene ring of the cinnamic acid can lead to different activities. The para ‐substitution on the benzene ring plays an important role in inhibiting JH biosynthesis in vitro . Moreover, M11 is considered to be a potential IGR for cockroach control. © 2016 Society of Chemical Industry
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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 | 0.001 | 0.001 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.003 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.001 | 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".