- Synthesis method of 3-methyl-2-benzothiazolinone hydrazone hydrochloride hydrate
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The invention discloses a synthesis method of a 3-methyl-2-benzothiazolinone hydrazone hydrochloride hydrate. According to the method, cheap and accessible 2-mercaptobenzothiazole is used as a starting raw material; 3-methyl-2-benzothiazolinone hydrazone is synthesized by a one-pot method; and a reaction is performed with hydrochloric acid to obtain the target product 3-methyl-2-benzothiazolinonehydrazone hydrochloride hydrate. The process is mild in reaction condition, high in yield, simple and convenient to operate, low in production cost, free of organic solvents, safe, reliable and suitable for large-scale production.
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Paragraph 0034; 0040-0054
(2020/04/02)
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- 3 - Methyl -2 - benzothiazolinone hydrazone hydrochloride salt and its hydrate synthesis method
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The present invention provides 3 - methyl - 2 - benzothiazolinone hydrazone hydrochloride salt and its hydrate synthesis method, which belongs to the field of organic synthesis. N - methylaniline with carbon disulfide reaction to obtain N - methyl - N - phenyl dithio-, then reaction with bromine 3 - methylbenzothiazol - 2 - thione, then reacting with hydrazine hydrate to produce 3 - methyl - 2 - benzothiazolinone hydrazone, subsequently react with hydrochloric acid to obtain 3 - methyl - 2 - benzothiazolinone hydrazone hydrochloride, recrystallization to obtain water in 3 - methyl - 2 - benzothiazolinone hydrazone hydrochloride hydrate. In the present invention the used raw materials are cheap and easily obtained, the operation process is simple, and has potential industrial amplifying application prospect.
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Paragraph 0016; 0017; 0018
(2019/01/08)
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- Design, synthesis and biological evaluation of novel unsymmetrical azines as quorum sensing inhibitors
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Targeting quorum sensing signals using quorum sensing inhibitors has opened new avenues for the application of known antibiotics. In this context, twenty five unsymmetrical azines were synthesised and evaluated as quorum sensing inhibitors. An efficient one-pot procedure was adopted that directly links 3-methyl-2-(methylthio)benzo[d]thiazol-3-ium salt, hydrazine hydrate and substituted aldehyde to give the designed compounds. The synthesized compounds were preliminarily tested for their potential to inhibit CviR receptor based QS signals in Chromobacterium violaceum. The bioassay screening results suggested that two compounds exhibited potent QS inhibition activity against CviR receptor, showing violacein inhibition (>50%) at 200 μM. Further, the putative positive hits were checked for their potential to inhibit LasR receptor-based QS using the PlasB-gfp(ASV) biomonitor strain of Pseudomonas aeruginosa. These compounds were found to inhibit the QS-mediated GFP signals in a dose dependant manner. Two active compounds also exhibited biofilm clearance at 50 μM concentration. Docking studies were performed to examine their potential to bind to the LasR protein of Pseudomonas aeruginosa.
- Chourasiya, Sumit S.,Kathuria, Deepika,Singh, Shaminder,Sonawane, Vijay C.,Chakraborti, Asit K.,Bharatam, Prasad V.
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p. 80027 - 80038
(2015/10/05)
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- Chemical Characterization of α-Oxohydrazone Ligation on Colloids: Toward Grafting Molecular Addresses onto Biological Vectors
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New mild and specific chemical strategies have been developed recently for the selective coupling of biological macromolecules. Among them, the hydrazone ligation strategy offers high chemoselectivity and versatility. We intended to use hydrazone ligation to target the controlled release of therapeutic agents by biological vectors (multilamellar vesicles called onion vectors). An accurate measure of ligation bond stability was needed to ensure that the ligation bond would stand long exposures to physiological conditions. In this study, we have completed a kinetic and thermodynamic characterization of hydrazone formation on a model reaction. The mechanism of the reaction in solution as well as in different self-organized systems (micelles, liposomes and multilamellar vesicles) was investigated. In solution, submicromolar stability was achieved as well as half-lives of several weeks. The kinetics and stability were both enhanced in colloidal media thanks to autoassociation effects. The results were expanded to the realistic case of RGD-peptide coupling to onion vectors. The RGD grafted onion vectors were then tested for their ability to bind endothelial cells in vitro.
- Chenevier,Bourel-Bonnet,Roux
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p. 16261 - 16270
(2007/10/03)
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- Test device comprising stable coupling dye for photometric determination of analytes
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A dye couple compound is provided for use in a test device containing a reagent system for detecting the presence or quantity of an analyte in a sample. The reagent system comprises one or more enzymes which, in the presence of the analyte, produce an oxidizing agent in quantities indicative of the quantity of analyte in the sample. The compound of choice is meta[3-methyl 2-benzothiazolinone hydrozone]N-sulfonyl benzenesulfonate monosodium.
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