- Synthesis and antimicrobial activity of dithiocarbamates of ω-Substituted (2-naphthyloxy)alkanes
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A series of dithiocarbamates of ω-substituted (2-naphthyloxy) alkanes was developed through condensation of 2-(2-chloro-alkoxy)-naphthalene to various kinds of aliphatic, aromatic, alicyclic, heterocyclic primary and secondary amines employing benzyl trimethyl ammonium hydroxide in catalytic quantity (Triton-B/CS2 system) afforded desired products in high yields (82-98 %). The complete series of synthesized compounds (4-48) were evaluated for antimicrobial activity through microdilution method using various bacterial and fungal strains. The antifungal and antibacterial values were estimated as MIC values. Fluconazole and ciprofloxacin [16 to 0.03 μg/ mL] were used as the standard antifungal and antibacterial drug, respectively. Out of series of evaluated compounds, some of these compounds such as compounds 28, 29, 30, 31, 32, 33 have displayed maximum potency which is comparable to standard drugs.
- Zaidi, Sadaf,Chaturvedi, Devdutt,Saxena, Mridula,Srivastava, Richa
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- Magnetic Nanoparticle Anchored Deep Eutectic Solvents as a Catalyst for the Etherification and Amination of Naphthols
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Herein, we introduce a reusable catalyst consisting of a deep eutectic solvent made up of choline chloride and p-toluene sulfonic acid (pTSA) covalently immobilized on magnetic nanoparticles (MNPs) as an agent for chemoselective direct ipso etherification and amination of naphthols. The bonding of the DES to the surface of the nanoparticles has increased the catalytic activity of the DES and also has simplified catalyst recovery from the reaction mixture. The MNP bound DES particles with an average size of 12±2 nm was characterized by FTIR, PXRD, HRTM, TGA, and VSM. For 16 tested etherification reactions, the functionalized magnetite nanoparticle catalyst gave an average yield of 84%; for 5 tested aminations the average yield was 77%. For all 23 tested reactions the yield was above 70% and pTSA Br?nsted acid loading was only 0.45 mol%. The catalytic performance could be attributed to the dispersion of the nanoparticles, strong DES-support interactions and interactions of the hydrogen donor species with naphthols. This work is the first catalytic examination of PDES covalently bonded on MNPs as a platform for organic transformations. (Figure presented.).
- Zamani, Parisa,Ozdemir, John,Ha, Yumi,Benamara, Mourad,Kuchuk, Adrian V.,Wang, Tengjiao,Chen, Jingyi,Khosropour, Ahmad R.,Beyzavi, M. Hassan
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supporting information
p. 4372 - 4380
(2018/10/15)
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- METHOD FOR PRODUCING POTASSIUM SALT, AND POTASSIUM SALT
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PROBLEM TO BE SOLVED: To provide a method that makes it possible to efficiently produce a halogen compound useful as a precursor of a compound that can be used suitably for optical materials in general. SOLUTION: A method for producing potassium salt includes the step for producing potassium salt represented by formula (1) by the reaction between a compound represented by formula (3), a cyclic carbonate ester compound, and potassium carbonate. [R2 is an aromatic ring-containing group having C constituting an aromatic ring at a binding site to O; n is 1 or 2; R1 independently represents an alkylene group]. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0059
(2018/04/10)
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- Design, synthesis, and systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake
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Two series of 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers were designed based on structure-activity relationship (SAR) and docking model of reported monoamine neurotransmitters reuptake inhibitors. The compounds were synthesized in 3-simple steps and their biological activities were evaluated. Several compounds were proven to be potent inhibitors of serotonin and norepinephrine reuptake. Computer docking was performed to study the interaction of the most potent compound 35 with human serotonin transporter. The results of the analyses suggest that 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers might be promising antidepressants worthy of further studies.
- Paudel, Suresh,Min, Xiao,Acharya, Srijan,Khadka, Daulat Bikram,Yoon, Goon,Kim, Kyeong-Man,Cheon, Seung Hoon
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p. 5538 - 5546
(2018/10/09)
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- MANUFACTURING METHOD OF HALOGEN COMPOUND, MANUFACTURING METHOD OF POTASSIUM SALT AND POTASSIUM SALT
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PROBLEM TO BE SOLVED: To provide a method capable of manufacturing a halogen compound useful as a precursor of a compound capable of being preferably used especially for optical system materials generally with high efficiency. SOLUTION: There is provided a manufacturing method of a halogen compound including a process of reacting a compound represented by the following formula (1) and a halogenation agent to produce a halogen compound represented by the following formula (2). In the formula (1), R1 is a linear or branched alkylene group, R2 is an aromatic ring-containing group having a carbon atom constituting an aromatic ring at a binding part with an oxygen atom represented in the formula, n is 1 or 2 and two of R1s may same or different when n is 2. In the formula (2), X is a halogen atom. COPYRIGHT: (C)2016,JPOandINPIT
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- Ortho-phenylenediamine-based open and macrocyclic receptors in selective sensing of H2PO4-, ATP and ADP under different conditions
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Ortho-phenylenediamine-based open and macrocyclic receptors have been designed and synthesized. The open receptor 1 and the macrocyclic receptor 2 fluorimetrically distinguish H2PO4- from the other anions examined in CH3CN with appreciable binding constant values. As practical applications, they are also sensible to nucleotides in aq. CH3CN (1:1, v/v). The receptor 1 shows significant emission change upon complexation of ATP and ADP. ADP is selectively distinguished by a ratiometric change in emission. In contrast, the macrocyclic receptor 2, under similar conditions, shows good binding with ATP over the others.
- Ghosh, Kumaresh,Saha, Indrajit
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p. 9383 - 9392
(2013/01/15)
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- ω-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents
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ω-(2-Naphthyloxy) amino alkanes, obtained as major by-product during course of synthesis of carbamate esters from ω-(2-naphthyloxy) alkyl halides and amines, showed significant anti-hyperglycemic and lipid lowering activities in various test models as a novel class of compounds. Compounds were tested in rat GLM, SLM, STZ, and STZ-S models at 100 mg/kg dose. Of these compound 13 was found to be the most active which caused lowering of sugar by 33.6%, 31.0%, 28.5%, and 73.8% in GLM, SLM, STZ, STZ-S, and db/db mice models, respectively. It also significantly effected lowering of LDL in rat model and also in Hamster model without reducing HDL. Most of the compounds showing anti-diabetic and lipid lowering activity have shown promising PPAR-α/γ/δ-activity. Compounds 6, 13, and 19 have shown very good PPAR-α/γ/δ activity.
- Chaturvedi, Devdutt,Ray, Suprabhat,Srivastava, Arvind K.,Chander, Ramesh
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p. 2489 - 2498
(2008/09/21)
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- OMEGA-SUBSTITUTED-NAPHTHYLOXYALKLAMINO DERIVATIVES AS ANTIHYPERGLYCEMIC AGENTS AND PREPARATION
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This invention relates to novel o-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid-lowering effects.
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Page/Page column 11
(2008/06/13)
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- Alpha-substituted naphthyloxy omega-substituted alkyl/aryl amino-substituted alkane derivatives as agent for treatment or prophylaxis of diabetes and related metabolic disorders
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This invention relates to novel {overscore (ω)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.
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