- Azobenzene-Semicarbazone Enables Optical Control of Insect Sodium Channels and Behavior
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Photopharmacology uses molecular photoswitches to establish control over the action of bioactive molecules. The application of photopharmacology in the research of invertebrate sodium channels has not been investigated. Here we report several photochromic ligands of metaflumizone. One ligand, termed ABM04, underwent reversible trans-cis isomerization under ultraviolet or blue light irradiation. cis-ABM04 had excellent larvicidal activity against mosquito larvae with an LC50 value of 4.39 μM and showed insecticidal activity against Mythimna separata with an LC50 value of 7.19 μM. However, trans-ABM04 was not found to have biological activity. ABM04 (10 μM) can induce depolarization of dorsal unpaired median neurons and enable the real-time photoregulation of mosquito larval behavior. The precise regulation of invertebrate sodium channels is realized for the first time, which provides a new strategy for the basic and accurate research of invertebrate sodium channels.
- Chen, Ruijia,Fu, Wen,Li, Zhong,Qiao, Zhi,Shao, Xusheng,Xu, Zhiping,Zhang, Yongchao
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p. 15554 - 15561
(2021/12/27)
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- A clean efficient cyanogen fluorine insect zong synthesis process (by machine translation)
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The invention relates to a clean efficient cyanogen fluorine insect zong synthesis process, comprising the following steps: The compounds of formula I with the compound of formula II in an organic solvent, under the action of a catalyst, the reaction produces cyanogen fluorine insect zong. (by machine translation)
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Paragraph 0017-0019
(2018/07/06)
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- Synthesis method of indoxacarb intermediate semicarbazone
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The invention discloses a synthesis method of an indoxacarb intermediate semicarbazone. The synthesis method includes the steps of producing 4-trifluoromethoxy phenylurea from 4-trifluoromethoxyaniline and isocyanate under the action of acetic acid; enabling the 4-trifluoromethoxy phenylurea and hydrazine hydrate to undergo hydrazinolysis in an organic solvent so as to obtain 4-trifluoromethoxy phenylamino hydrazide; enabling the 4-trifluoromethoxy phenylamino hydrazide and 5-chloro-1,3-dihydro-2-hydroxy-1-oxo-2H-indene-2-carboxylic acid methyl ester in an organic solvent under the action of a catalyst. The synthesis method has the advantages that the intermediate semicarbazone is synthesized from industrially available isocyanate through a series of conversion, and accordingly the synthesis method is free of toxic substances and phosgene products and capable of avoiding the shortcomings of high cost and low yield when precious metals serve as catalysts as well as overcoming the technical defect of low ring-closure reaction yield; the synthesis method is high in safety and is economical and high in yield when used for synthesizing indoxacarb atoms.
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- Optically active antifungal azoles. VI. Synthesis and antifungal activity of N-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl) propyl]-N′-(4-substituted phenyl)-3(2H,4H)-1,2,4-triazolones and 5(1H,4H)-tetrazolones
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A new series of optically active antifungal azoles, N-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl) propyl]-N′-(4-substituted phenyl)-3(2H,4H)-1,2,4-triazolones (1,2) and 5(1H,4H)-tetrazolones (3), were prepared from the triflate derivative of (1S)-1-[(2R)-2-(2,4-difluorophenyl)-2-oxiranyl]ethanol (13) by an SN2 displacement reaction with the union of an azolone (17-19) and subsequent ring-opening reaction with 1H-1,2,4-triazole. The optically active oxiranylethanol 13 was synthesized from methyl (R)-lactate in a stereocontrolled manner. The azolones 1-3 prepared showed potent antifungal activities in vitro and in vivo.
- Kitazaki, Tomoyuki,Tamura, Norikazu,Tasaka, Akihiro,Matsushita, Yoshihiro,Hayashi, Ryogo,Okonogi, Kenji,Itoh, Katsumi
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p. 314 - 327
(2007/10/03)
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