88138-52-7Relevant academic research and scientific papers
Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker
Abdelhameed, Ahmed,Feng, Mei,Joice, April C.,Zywot, Emilia M.,Jin, Yiru,La Rosa, Chris,Liao, Xiaoping,Meeds, Heidi L.,Kim, Yena,Li, Junan,McElroy, Craig A.,Wang, Michael Zhuo,Werbovetz, Karl A.
, p. 1901 - 1922 (2021/02/22)
Due to the limitations of existing medications, there is a critical need for new drugs to treat visceral leishmaniasis. Since arylimidamides and antifungal azoles both show oral activity in murine visceral leishmaniasis models, a molecular hybridization approach was employed where arylimidamide and azole groups were separated by phenoxyalkyl linkers in an attempt to capitalize on the favorable antileishmanial properties of both series. Among the target compounds synthesized, a greater antileishmanial potency against intracellular Leishmania donovani was observed as the linker length increased from two to eight carbons and when an imidazole ring was employed as the terminal group compared to a 1,2,4-triazole group. Compound 24c (N-(4-((8-(1H-imidazol-1-yl)octyl)oxy)-2-isopropoxyphenyl) picolinimidamide) displayed activity against L. donovani intracellular amastigotes with an IC50 value of 0.53 μM. When tested in a murine visceral leishmaniasis model, compound 24c at a dose of 75 mg/kg/day p.o. for five consecutive days resulted in a modest 33% decrease in liver parasitemia compared to the control group, indicating that further optimization of these molecules is needed. While potent hybrid compounds bearing an imidazole terminal group were also strong inhibitors of recombinant CYP51 from L. donovani, as assessed by a fluorescence-based assay, additional targets are likely to play an important role in the antileishmanial action of these compounds.
NOVEL LUMINESCENT LANTHANIDE CHELATE REPORTERS, BIOSPECIFIC BINDING REACTANTS LABELLED WITH NOVEL LUMINESCENT LANTHANIDE CHELATE REPORTERS AND THEIR USE
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Page/Page column 42; 43; 60, (2021/01/23)
The present invention relates to novel luminescent lanthanide chelate reporters which are formed from two to three separate lanthanide chelate moieties covalently conjugated to each other to act as an unique labelling reactant, and which can be attached to a biospecific reactant and used in various assays.
Discovery of Diphenoxy Derivatives with Flexible Linkers as Ligands for β-Amyloid Plaques
Jia, Jianhua,Zhang, Longfei,Song, Jia,Dai, Jiapei,Cui, Mengchao
, p. 4089 - 4100 (2020/12/13)
The highly rigid and planar scaffolds with π-conjugated systems have been widely considered to be indispensable for β-amyloid (Aβ) binding ligands. In this study, a library of diphenoxy compounds with different types of more flexible linkers as Aβ ligands were synthesized and evaluated. Most of them displayed good affinity (Ki1-42aggregates, and some ligands even showed values of Kiless than 10 nM. Structure-activity relationship analysis revealed that modification on the linkers or substituents tolerated great flexibility, which challenged the long-held belief that rigid and planar structures are exclusively favored for Aβ binding. Three ligands were labeled by iodine-125, and they exhibited good properties in vitro and in vivo, which further supported that this flexible scaffold was potential and promising for the development of Aβ imaging agents.
Diphenoxyl flexible molecules with high affinity with A[beta] plaque and preparation method and applications thereof
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Paragraph 0073; 0074; 0085; 0086, (2017/12/09)
The invention discloses diphenoxyl flexible molecules with high affinity with A[beta] plaque and a preparation method and applications thereof. After the molecules are labeled by radionuclide, the molecules can be used as an A[beta] plaque developing agen
Alignment of palladium complexes into columnar liquid crystals driven by peripheral triphenylene substituents
Tritto, Emiliano,Chico, Ruben,Sanz-Enguita, Gerardo,Folcia, Cesar L.,Ortega, Josu,Coco, Silverio,Espinet, Pablo
supporting information, p. 3449 - 3455 (2014/05/06)
A new triphenylene-imine (ImH) and its ortho-palladated complexes (μ-X)2[Pd2Im2] (X = CH3COO -, Cl-, Br-), (μ-Cl)(μ-SC nH2n+1)[Pd2Im2]
Nitrosoarene dimerization on two- and three-dimensional gold surfaces
Biljan, Ivana,Medancic, Tina,Kralj, Marko,Radic, Tea Misic,Svetlicic, Vesna,Vancik, Hrvoj
, p. 83 - 94 (2013/07/27)
In the present study, we investigated nitrosoarene dimerization on an Au(111) and on the surface of gold nanoparticles (AuNPs). High-resolution STM images revealed that 8-thiocyanatooctyl-4-nitrosobenzoate (NCS(CH 2)8OOCC6
Comparative syntheses of arylamine monomer with styrylpyridyl photo-crosslinker of polyarylamine for OLED hole-injection material
Choi, Heung-Jin,Song, Moo-Gon,Sim, Youn-Hee,Bae, Heung-Kwon,Kim, Jin-Woo,Park, Lee Soon
experimental part, p. 47 - 54 (2011/08/02)
A new arylamine monomer with photo-crosslinkable styrylpyridinyl moiety of conjugated polyarylamine for OLED hole injection material was synthesized through two synthetic routes, BOC-amine protection/deprotection and nitro group reduction methods. Both sy
Hybrid ortho/allosteric ligands for the adenosine A1 receptor
Narlawar, Rajeshwar,Lane, J. Robert,Doddareddy, Munikumar,Lin, Judy,Brussee, Johannes,Ijzerman, Adriaan P.
supporting information; experimental part, p. 3028 - 3037 (2010/09/07)
Many G protein-coupled receptors (GPCRs), including the adenosine A 1 receptor (A1AR), have been shown to be allosterically modulated by small molecule ligands. So far, in the absence of structural information, the exact location of
