92013-18-8Relevant academic research and scientific papers
Synthesis and insecticidal activity of mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety
Pan, Jianke,Yu, Lu,Liu, Dengyue,Hu, Deyu
, (2018/05/30)
Mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety were designed, synthesized, and evaluated for their insecticidal activity. Some of the title compounds showed remarkable insecticidal properties against Aphis craccivora. Compound I13 exhibited satisfactory insecticidal activity against A. craccivora. Meanwhile, label-free proteomics analysis of compound I13 treatment identified a total of 821 proteins. Of these, 35 proteins were up-regulated, whereas 108 proteins were down-regulated. Differential expressions of these proteins reflected a change in cellular structure and metabolism.
APELIN RECEPTOR AGONISTS AND METHODS OF USE
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Page/Page column 116; 119, (2017/12/28)
The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
SUBSTITUTED BENZAMIDES AND THEIR USES
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Paragraph 0711, (2015/12/01)
Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
SUBSTITUTED BENZAMIDES AND THEIR USES
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Page/Page column 175, (2013/11/05)
Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
Design and synthesis of novel lactate dehydrogenase a inhibitors by fragment-based lead generation
Ward, Richard A.,Brassington, Claire,Breeze, Alexander L.,Caputo, Alessandro,Critchlow, Susan,Davies, Gareth,Goodwin, Louise,Hassall, Giles,Greenwood, Ryan,Holdgate, Geoffrey A.,Mrosek, Michael,Norman, Richard A.,Pearson, Stuart,Tart, Jonathan,Tucker, Julie A.,Vogtherr, Martin,Whittaker, David,Wingfield, Jonathan,Winter, Jon,Hudson, Kevin
supporting information; experimental part, p. 3285 - 3306 (2012/06/01)
Lactate dehydrogenase A (LDHA) catalyzes the conversion of pyruvate to lactate, utilizing NADH as a cofactor. It has been identified as a potential therapeutic target in the area of cancer metabolism. In this manuscript we report our progress using fragment-based lead generation (FBLG), assisted by X-ray crystallography to develop small molecule LDHA inhibitors. Fragment hits were identified through NMR and SPR screening and optimized into lead compounds with nanomolar binding affinities via fragment linking. Also reported is their modification into cellular active compounds suitable for target validation work.
INHIBITORS OF BETA-SECRETASE
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Page/Page column 76-77, (2010/10/03)
The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity
Musso, David L.,Cochran, Felicia R.,Kelley, James L.,McLean, Ed W.,Selph, Jeffrey L.,Rigdon, Greg C.,Orr, G. Faye,Davis, Ronda G.,Cooper, Barrett R.,Styles, Virgil L.,Thompson, James B.,Hall, William R.
, p. 399 - 408 (2007/10/03)
The design of rigid cyclic analogues derived from cinnamamide 1, (E)-N-cyclopropyl-3-(3-fluorophenyl)prop-2-enamide, and β-methylcinnamamide 2, (E)-N-cyclopropyl-3-(3-fluorophenyl)but-2-enamide, has led to the discovery of the potent, centrally acting muscle relaxant (E)-2-(4,6-difluoro-1-indanylidene)acetamide, 17. Compound 17 also possesses potent antiinflammatory and analgesic activity. This paper describes the synthesis and the muscle relaxant, antiinflammatory, and analgesic structure-activity relationships of 17 and 67 of its analogues. Compound 17 has been taken into phase I clinical trials.
Indenyl compounds for the polymerization of olefins
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Example II, (2010/01/30)
Indenyl compound of formula (1) wherein: M is a transition metal from the lanthanides or from group 3, 4, 5 or 6 of the Periodic System of Elements, Q is an anionic ligand to M, k is the number of Q groups, R is a bridging group and Z and X are substituents, wherein R contains at least one sp2-hybridized carbon atom that is bonded to the indenyl group at the 2-position with the exclusion of Ti(deshydronorbiphenacene) dichloride.
The effect of vinyl esters on the enantioselectivity of the lipase-catalysed transesterification of alcohols
Kawasaki, Masashi,Goto, Michimasa,Kawabata, Shigeki,Kometani, Tadashi
, p. 585 - 596 (2007/10/03)
The enantioselectivity of the lipase from Pseudomonas cepacia (PCL) in the transesterification of 2-phenyl-1-propanol 1 was studied using a series of vinyl 3-arylpropanoates as acyl donors. The most enantioselective transesterification reaction of the alcohol was attained by using vinyl 3-(p-iodophenyl)- or 3-(p-trifluoromethylphenyl)propanoates, with enantiomer ratios, E, of 116 and 138, respectively. Vinyl 3-phenylpropanoate was also effective for the resolution of 1 mediated by lipases from P. fluorescens and porcine pancreas and for the PCL-catalysed transesterification of several 2-phenyl-1-alkanols. The enantiomeric resolution of 1 was practically carried out by the first enantioselective transesterification using PCL and vinyl 3-(p-iodophenyl)propanoate to afford (R)-1 and then the enantioselective hydrolysis of the resultant ester to afford (S)-1.
Synthesis of Biological Markers in Fossil Fuels. 2. Synthesis and 13C NMR Studies of Substituted Indans and Tetralins
Adamczyk, Maciej,Watt, David S.,Netzel, Daniel A.
, p. 4226 - 4237 (2007/10/02)
Unambiguous syntheses of all possible methyl, ethyl, n-propyl, and n-butyl derivatives of indan and tetralin were developed using the Kumada coupling procedure involving the reaction of aryl or vinyl halides with Grignard reagents in the presence of nickel(II) chloride.An analysis of the 13C NMR spectra of these compounds was also completed.
