Liu, Jingbo published the artcileDiscovery of a polysubstituted phenyl containing novel N-phenylpyrazole scaffold as potent ryanodine receptor activator, Recommanded Product: 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine, the publication is Bioorganic & Medicinal Chemistry (2020), 28(24), 115829, database is CAplus and MEDLINE.
To develop the novel ryanodine receptors (RyRs) insecticides, encouraged by our previous research work, a series of novel N-phenylpyrazole derivatives containing a polysubstituted Ph ring scaffold were designed and synthesized. The bioassays results indicated that some title compounds exhibited excellent insecticidal activity. For oriental armyworm (Mythimna separata), compounds (I), (II), (III) and (IV) at 0.5 mg L-1 displayed 100% larvicidal activity, and even at 0.1 mg L-1, 7o was 30% larvicidal activity, comparable to chlorantraniliprole (30%) and better than cyantraniliprole (10%). Compounds I and IV had the median lethal concentrations (LC50) of 8.83 × 10-2 and 7.12 × 10-2 mg L-1, resp., close to chlorantraniliprole (6.79 × 10-2 mg L-1). Addnl., for diamondback moth (Plutella xylostella), the larvicidal activity of compounds I and III were 90% and 70% at 0.01 mg L-1, resp., better than chlorantraniliprole (50%) and cyantraniliprole (40%). More impressively, the LC50 value of 7f was 4.2 × 10-3 mg L-1, slightly lower than that of chlorantraniliprole (5.0 × 10-3 mg L-1). The mol. docking between compound I and RyRs of diamondback moth validated our mol. designation. Furthermore, the calcium imaging experiment explored the influence of compound IV on the calcium homeostasis in the central neurons of the third larvae of oriental armyworm. The results of this study indicated that IV is a potent novel lead targeting at RyRs.
Bioorganic & Medicinal Chemistry published new progress about 1869-22-3. 1869-22-3 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Hydrazine,Amine,Benzene, name is 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine, and the molecular formula is C7H6ClF3N2, Recommanded Product: 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine.
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https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics