Xie, Yong published the artcileSynthesis, Biological Activity, and Conformational Study of N-Methylated Allatostatin Analogues Inhibiting Juvenile Hormone Biosynthesis, Recommanded Product: (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, the publication is Journal of Agricultural and Food Chemistry (2015), 63(11), 2870-2876, database is CAplus and MEDLINE.
An allatostatin (AST) neuropeptide mimic (H17) is a potential insect growth regulator, which inhibits the production of juvenile hormone (JH) by the corpora allata. To determine the effect of conformation of novel AST analogs and their ability to inhibit JH biosynthesis, eight insect AST analogs were synthesized using H17 as the lead compound by N-methylation scanning, which is a common strategy for improving the biol. properties of peptides. A bioassay using JH production by corpora allata of the cockroach Diploptera punctata indicated that single N-methylation mimics (analogs 1-4) showed more activity than double N-methylation mimics (analogs 5-8). Especially, analogs 1 and 4 showed roughly equivalent activity to that of H17, with IC50 values of 5.17 × 10-8 and 6.44 × 10-8 M, resp. Mol. modeling based on NMR data showed that the conformation of analogs 1 and 4 seems to be flexible, whereas analogs 2 and 3 showed a type IV β-turn. This flexible linear conformation was hypothesized to be a new important and indispensable structural element beneficial to the activity of AST mimics.
Journal of Agricultural and Food Chemistry published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C12H17NO2, Recommanded Product: (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid.
Referemce:
https://en.wikipedia.org/wiki/Ether,
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