929193-49-7Relevant articles and documents
2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds and preparation method thereof
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Paragraph 0157; 0159-0161, (2017/08/02)
The invention discloses 2'-carbonyl-3-bromo-spiro[benzofuran-2, 4'-oxazolidine] compounds and a preparation method thereof. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive compounds shown in the structural formula II. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive spiro compounds, photoactive chiral spiro compounds with multiple functional groups substituted, such as photoactive chiral spiro compounds with azido groups, hydroxyl groups, allyl groups and anisole groups substituted, can be obtained through substitution reactions of bromine atoms at site 3 under different reaction conditions. Therefore, different kinds of other photoactive chiral spiro compounds are prepared by using the substitution reactions of bromine atoms, the range of the compounds is enlarged, and the potential application value is great.
Bicyclic aromatic substituted pyridone derivative
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Page/Page column 49, (2009/10/30)
Disclosed is a compound represented by the formula (I): Wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, —O— or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl) heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists
Newman, Amy Hauck,Grundt, Peter,Cyriac, George,Deschamps, Jeffrey R.,Taylor, Michelle,Kumar, Rakesh,Ho, David,Luedtke, Robert R.
experimental part, p. 2559 - 2570 (2010/03/01)
In the present report, the D3 receptor pharmacophore is modified in the 2,3-diCl- and 2-OCH3-phenyl-piperazine class of compounds with the goal to improve D3 receptor affinity and selectivity. This extension of structure-activity relationships
Evaluation of radiolabeled (Hetero)aromatic analogues of N-(2-diethylaminoethyl)-4-iodobenzamide for imaging and targeted radionuclide therapy of melanoma
Chezal, Jean-Michel,Papon, Janine,Labarre, Pierre,Lartigue, Claire,Galmier, Marie-Josephe,Decombat, Caroline,Chavignon, Olivier,Maublant, Jean,Teulade, Jean-Claude,Madelmont, Jean-Claude,Moins, Nicole
experimental part, p. 3133 - 3144 (2009/04/07)
Targeted radionuclide therapy using radioiodinated compounds with a specific affinity for melanoma tissue is a promising treatment for disseminated melanoma, but the candidate with the ideal kinetic profile remains to be discovered. Targeted radionuclide therapy concentrates the effects on tumor cells, thereby increasing the efficacy and decreasing the morbidity of radiotherapy. In this context, analogues of N-(2-diethylaminoethyl)-4- iodobenzamide (BZA) are of interest. Various (hetero)aromatic analogues 5 of BZA were synthesized and radioiodinated with 125I, and their biodistribution in melanoma-bearing mice was studied after i.v. administration. Most [125I]5-labeled compounds appeared to bind specifically and with moderate-to-high affinity to melanoma tumor. Two compounds, 5h and 5k, stood out with high specific and long-lasting uptake in the tumor, with a 7- and 16-fold higher value than BZA at 72 h, respectively, and kinetic profiles that makes them promising agents for internal targeted radionuclide therapy of melanoma.
Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
Byun, Ji Hun,Kim, HyeYun,Kim, YoungSoo,Mook-Jung, Inhee,Kim, Dong Jin,Lee, Won Koo,Yoo, Kyung Ho
scheme or table, p. 5591 - 5593 (2009/06/18)
The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
BICYCLIC AROMATIC SUBSTITUTED PYRIDONE DERIVATIVE
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Page/Page column 80, (2010/11/26)
Disclosed is a compound represented by the formula (I): wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, -O- or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methlene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.