- Tunable aryl imidazolium ionic liquids (TAIILs) as environmentally benign catalysts for the esterification of fatty acids to biodiesel fuel
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Herein, we describe the synthesis of tunable aryl imidazolium ionic liquid catalysts and tested for esterification of fatty acids to biodiesel. In this work, six tunable aryl imidazolium ionic liquids (TAIILs) 1a-1f were prepared. These ionic liquids were used as the economical and reusable catalysts for the synthesis of biodiesel fuels. The reaction has been preceded in a monophase at 80 °C for 4 h, after which the product was separated from the catalyst system by a simple liquid/liquid phase separation at room temperature with excellent yields. With the simple post-process, the catalyst is reusable at least 6 times. This novel method offers a short reaction time, good yields, and environmentally benign characteristics.
- Ho, Wen-Yueh,Lin, Wesley,Lin, Yi-Jyun,Luo, Shun-Yuan,Pantawane, Amit,Su, Po-Fang,Thul, Mayur,Tseng, Shao-An,Wu, Hsin-Ru
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- 1,2,4-oxadiazole-based bio-isosteres of benzamides: Synthesis, biological activity and toxicity to zebrafish embryo
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To discover new compounds with broad spectrum and high activity, we designed a series of novel benzamides containing 1,2,4-oxadiazole moiety by bioisosterism, and 28 benzamides derivatives with antifungal activity were synthesized. These compounds were ev
- Yang, Sen,Ren, Chao-Li,Ma, Tian-Yang,Zou, Wen-Qian,Dai, Li,Tian, Xiao-Yu,Liu, Xing-Hai,Tan, Cheng-Xia
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- Synthesis and biological activity of benzamides substituted with pyridine-linked 1,2,4-oxadiazole
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To find pesticidal lead compounds with high activity, a series of novel benzamides substituted with pyridine-linked 1,2,4-oxadiazole were designed by bioisosterism, and synthesized easily via esterification, cyanation, cyclization and aminolysis reactions
- Dai, Li,Liu, Xing-Hai,Ma, Tian-Yang,Mei, Jun-Chang,Ren, Chao-Li,Tan, Cheng-Xia,Tian, Xiao-Yu,Yang, Sen
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- 1,2,4-oxadiazole bipyridine substituted benzamide compound as well as preparation method and application thereof
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The invention belongs to the technical field of chemical synthesis and drug application, and particularly relates to a 1,2,4-oxadiazole bipyridine substituted benzamide compound as well as a preparation method and application thereof. The preparation meth
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Paragraph 0024-0026
(2020/09/08)
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- Novel bifenthrin derivatives, and preparation method and application thereof
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The invention discloses novel bifenthrin derivatives, and a preparation method and application thereof. The novel bifenthrin derivatives have a structural formula as shown in a formula (I) which is described in the specification. In the formula (I), when R1 is H, R2 is a Cl or CF3 substituent group, and R3 is H or a substituted or unsubstituted non-heterocyclic or heterocyclic aryl group; when R1is a Cl substituted group, R 2 is H or a Cl or CF3 substituent group, and R3 is H or a substituted or unsubstituted non-heterocyclic or heterocyclic aryl group; the non-heterocyclic aryl group is a phenyl, naphthyl, anthryl, phenanthryl or pyrenyl group; and the heterocyclic aryl group is a five-to-nine-membered monocyclic or polycyclic heterocyclic aryl group with one or more O or S heteroatoms.According to the invention, a series of the novel bifenthrin derivatives are synthesized mainly by modifying and transforming ortho-position and terminal-position benzene rings on the intermediate benzene rings of bifenthrin; and the novel bifenthrin derivatives have excellent insecticidal and mosquito-killing effect on both larvae and adult mosquitoes, are significantly reduced in toxicity and improved in metabolic stability, and shows good application prospects.
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- Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists
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Ghrelin plays a major physiological role in the control of food intake, and inverse agonists of the ghrelin receptor (GHS-R1a) are widely considered to offer utility as antiobesity agents by lowering the set-point for hunger between meals. We identified an acylurea series of ghrelin modulators from high throughput screening and optimized binding affinity through structure-activity relationship studies. Furthermore, we identified specific substructural changes, which switched partial agonist activity to inverse agonist activity, and optimized physicochemical and DMPK properties to afford the non-CNS penetrant inverse agonist 22 (AZ-GHS-22) and the CNS penetrant inverse agonist 38 (AZ-GHS-38). Free feeding efficacy experiments showed that CNS exposure was necessary to obtain reduced food intake in mice, and it was demonstrated using GHS-R1a null and wild-type mice that this effect operates through a mechanism involving GHS-R1a.
- McCoull, William,Barton, Peter,Brown, Alastair J. H.,Bowker, Suzanne S.,Cameron, Jennifer,Clarke, David S.,Davies, Robert D. M.,Dossetter, Alexander G.,Ertan, Anne,Fenwick, Mark,Green, Clive,Holmes, Jane L.,Martin, Nathaniel,Masters, David,Moore, Jane E.,Newcombe, Nicholas J.,Newton, Claire,Pointon, Helen,Robb, Graeme R.,Sheldon, Christopher,Stokes, Stephen,Morgan, David
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supporting information
p. 6128 - 6140
(2014/08/18)
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- BENZAMIDE INHIBITORS OF THE P2X7 RECEPTOR
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The present invention provides benzamide inhibitors of the P2X7 receptor of the formula (I), wherein R1 -R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, incl
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