87477-66-5Relevant 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.
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.
Synthesis of pure blue emissive poly(2,7-carbazole)s anchored by electron donor pendant
Inada, Takashi,Shinnai, Toshinobu,Kijima, Masashi
, p. 2526 - 2534 (2019/11/03)
Three novel poly(2,7-carbazole)s having hole injection and transporting pendent moieties of carbazole and triphenylamine at the N-position were synthesized for achieving pure blue electroluminescence. The N-pendants in the polymers correspond to N-phenylcarbazol-2-yl (P1), N,N-diphenylamino-N-phenylcarabazol-2-yl (P2), and 4-phenyl having a hydrocarbon chain with a triphenylamine terminal (P3), respectively. Electronic, optical, and electroluminescence properties of these polymers were compared with those of a poly(2,7-carbazole) directly connected with triphenylamine at the N-position (P0) having an aggregation-induced emissive property. The photoluminescence (PL) spectra suggested that they could emit in the region of blue light in the film state. Especially, P2 that has the fixed and large diphenylaminocarbazolyl pendant showed a deep-blue fluorescence with CIE(x, y) = (0.15, 0.07). The P0, P2, and P3 based light emitting diode devices showed maximum electroluminescence wavelengths in the range of 430–450 nm. The P2 device showed pure blue emission (CIE[x, y] = [0.18, 0.16]), high luminance (1130 cd/m2) and current density (628 mA/cm2) at 8 V, whereas low-energy emissions around 500–600 nm were emerged at higher than 9 V. The P0 and P3 devices also showed a blue electroluminescence in the range of 8–11 V, but their luminance and efficiency were low.
Diphenoxyl flexible molecules with high affinity with A[beta] plaque and preparation method and applications thereof
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Paragraph 0073; 0074; 0091; 0092, (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
A new supramolecular sulfonated polyimide for use in proton exchange membranes for fuel cells
Ye, Yun-Sheng,Huang, Yao-Jheng,Cheng, Chih-Chia,Chang, Feng-Chih
supporting information; experimental part, p. 7554 - 7556 (2010/12/19)
Uracil-terminated telechelic sulfonated polyimides (SPI-U) were transformed into noncovalent network membranes through biocomplementary hydrogen bonding recognition in the presence of an adenine-based crosslinking agent. SPI-U membrane exhibited dramatica
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
Fabrication and fluorescence properties of perylene bisimide dye aggregates bound to gold surfaces and nanopatterns
Haas, Ulrike,Thalacker, Christoph,Adams, Joerg,Fuhrmann, Juergen,Riethmueller, Silke,Beginn, Uwe,Ziener, Ulrich,Moeller, Martin,Dobrawa, Rainer,Wuerthner, Frank
, p. 767 - 772 (2007/10/03)
Perylene bisimide dyes with two different imide substituents have been synthesized by sequential imidization reactions to give the disulfide 8 bearing two perylene bisimide dyes. Aggregation properties of this bis-perylene dye were studied by UV/Vis absor
Bifunctional Reactivity of the Nitrophenoxyl Group in Intramolecular Photoreactions
Mutai, Kiyoshi,Tukada, Hideyuki,Nakagaki, Ryoichi
, p. 4896 - 4903 (2007/10/02)
The photochemical behavior of a homologous series of compounds, p-O2NC6H4O(CH2)nNHPh (n = 2-10, 12, and 16) in acetonitrile is reported.The lower (n = 2-6) homologues undergo an apparently nucleophilic type rearrangement to give ω-((p-nitrophenyl)amino)al
