101871-81-2Relevant articles and documents
Helical polycarbodiimide cloaking of carbon nanotubes enables inter-nanotube exciton energy transfer modulation
Budhathoki-Uprety, Januka,Jena, Prakrit V.,Roxbury, Daniel,Heller, Daniel A.
, p. 15545 - 15550 (2014)
The use of single-walled carbon nanotubes (SWCNTs) as near-infrared optical probes and sensors require the ability to simultaneously modulate nanotube fluorescence and functionally derivatize the nanotube surface using noncovalent methods. We synthesized a small library of polycarbodiimides to noncovalently encapsulate SWCNTs with a diverse set of functional coatings, enabling their suspension in aqueous solution. These polymers, known to adopt helical conformations, exhibited ordered surface coverage on the nanotubes and allowed systematic modulation of nanotube optical properties, producing up to 12-fold differences in photoluminescence efficiency. Polymer cloaking of the fluorescent nanotubes facilitated the first instance of controllable and reversible internanotube exciton energy transfer, allowing kinetic measurements of dynamic self-assembly and disassembly.
Synthesis, evaluation, and molecular docking studies of aryl urea-triazole-based derivatives as anti-urease agents
Moghimi, Setareh,Goli-Garmroodi, Fereshteh,Allahyari-Devin, Maryam,Pilali, Hedieh,Hassanzadeh, Malihe,Mahernia, Shabnam,Mahdavi, Mohammad,Firoozpour, Loghman,Amanlou, Massoud,Foroumadi, Alireza
, (2018)
Considering the importance of urease inhibitors in the treatment of ureolytic bacterial infections, in this work, the synthesis of novel, aryl urea-triazole-based derivatives as effective urease inhibitors is described. Dichloro-substituted derivative 4o,
2,2,2-Trifluroenthanol promoted synthesis of unsymmetrical ureas from dioxazolones and amines via tandem lossen rearrangement/condensation process
Li, Jian,He, Wang,Lei, Pan,Song, Jiacheng,Huo, Jiyou,Wei, Hongbo,Bai, Hongjin,Xie, Weiqing
supporting information, p. 3590 - 3600 (2021/10/07)
A 2,2,2-trifluroenthanol (TFE) promoted synthesis of unsymmetric ureas was described. This approach enabled the construction of a variety of ureas from the readily prepared and easy-to-handle dioxazolones and amines via tandem Lossen rearrangement/condensation process. The reaction featured mild conditions for the urea synthesis under metal-free conditions, which was successively applied in the scale-up synthesis of herbicides Monuro and Isoproturon.
A three-component, Zn(OTf)2-mediated entry into trisubstituted 2-aminoimidazoles
Lukin, Alexei,Bakholdina, Anna,Kryukova, Anna,Sapegin, Alexander,Krasavin, Mikhail
supporting information, p. 1061 - 1064 (2019/06/08)
A three-component reaction involving in situ generation of propargylureas and subsequent Zn(OTf)2-mediated cyclocondensation with a primary amine yielded trisubstituted 2-aminoimidazoles. These findings are in contrast to the previously reporte
HELICAL POLYCARBODIIMIDE POLYMERS AND ASSOCIATED IMAGING, DIAGNOSTIC, AND THERAPEUTIC METHODS
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Paragraph 0186, (2016/03/16)
Described herein are suspensions of helical polycarbodiimide polymers that 'cloak' nanotubes, thereby effecting control over nanotube emission, providing a new mechanism of environmental responsivity, and enabling precise control over sub-cellular localiz
Electrophile-Mediated Reactions of Functionalized Propargylic Substrates
Urbanaite, Aurelija,Jonu?is, Mantas,Buk?naitiene, Rita,Balkaitis, Simonas,?ikotiene, Inga
supporting information, p. 7091 - 7113 (2015/11/16)
Metal-free halogen, chalcogen, or oxocarbenium ion mediated yne-carbonyl or yne-thioxo transformations of a range of N- and O-propargylic compounds have been studied. This investigation has led to the development of a mild, economic, and effective method for the synthesis of functionalized 4H-1,3-oxazines, 4H-1,3-thiazines, 4,5-dihydrothiazoles, and α-substituted enones. The structure of the propargylic substrate and the nature of electrophile influence both the outcome and regioselectivity of processes. Metal-free electrophile-mediated transformations of various N- and O-propargylic compounds have been studied. The scope and limitations of these reactions have been evaluated by using a broad range of substrates.
Novel VEGFR-2 kinase inhibitors identified by the back-to-front approach
Sanphanya, Kingkan,Wattanapitayakul, Suvara K.,Phowichit, Suwadee,Fokin, Valery V.,Vajragupta, Opa
supporting information, p. 2962 - 2967 (2013/06/27)
We report a novel VEGFR-2 inhibitor, developed by the back-to-front approach. Docking experiments indicated that the 3-chloromethylphenylurea motif of the lead compound occupied the back pocket of VEGFR-2 kinase. An attempt was made to enhance the binding affinity of 1 by expanding the structure to access the front pocket using a triazole linker. A library of 1,4-(disubstituted)-1H-1, 2,3-triazoles were screened in silico, and one compound (VH02) was identified with an IC50 against VEGFR-2 of 0.56 μM. VH02 showed antiangiogenic effects, inhibiting tube formation in HUVEC cells (EA.hy926) at 0.3 μM, 13 times lower than its cytotoxic dose. These enzymatic and cellular activities suggest that VH02 has potential as a lead for further optimization.
Synthesis and evaluation of 1-(substituted)-3-prop-2-ynylureas as antiangiogenic agents
Sanphanya, Kingkan,Wattanapitayakul, Suvara K.,Prangsaengtong, Orawin,Jo, Michiko,Koizumi, Keiichi,Shibahara, Naotoshi,Priprem, Aroonsri,Fokin, Valery V.,Vajragupta, Opa
supporting information; experimental part, p. 3001 - 3005 (2012/06/04)
Novel urea derivatives of alkynes have been designed, synthesized, and evaluated as potential cancer therapeutics leads. The most active 1-((3-chloromethyl)phenyl)-3-prop-2-ynylurea (1) exhibited cytotoxic effect against HELA and MCF-7 cell lines with IC50 values of 1.55 μM and 1.48 μM, respectively. Further investigation on tube formation assay in human vein umbilical cells (HUVEC) demonstrated that 1 and methyl 4-(3-(3-ethynylureido)benzyloxy) benzoate (6) possess antiangiogenic activity, with minimum effective dose of 25 nM (for 1) and 6.25 μM (for 6). The ED 50 of 1 and 6 were found to be 0.26 μM and 17.52 μM, respectively. The results from in vitro tyrosine kinase assay indicated the EGFR inhibition of 1 over other kinases (VEGFR2, FGFR1 and PDGFRβ). The cytotoxicity of 1 against EGFR overexpressing cell line A431 (IC50 36 nM) was comparable to that of erlotinib. The binding mode of 1 from docking simulation in the EGFR active site revealed that the urea motif formed hydrogen bonding with Lys745, Thr854 and Asp855 in hydrophobic pocket of EGFR. Compound 1 is considered as a potential lead for further optimization.
SUBSTITUTED SULFONAMIDO-MACROCYCLES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISINGS SAME, METHODS OF PREPARING SAME AND USES SAME
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Page/Page column 44; 49-50, (2008/06/13)
The invention relates to substituted sulfonamido-macrocycles according to the general formula (I): in which R1, R2, R4, R5, A, B, C, L, X, Y, Z, n, and m are as defined in the claims, and salts, N-oxides, or sol
IMIDAZOLE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION THEREOF
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, (2008/06/13)
A compound of formula (I) the process of preparing compounds of formula (I), their pharmaceutical compositions, and the method of treating diseases associated with M 3 muscarinic and/or S--HT 4 serotoninergic receptors.