cas 4300-43-0, N,N′-BIS-(3,4-DICHLOROPHENYL)UREA

Articles about 4300-43-0Total 9 be found

QSAR and classification of murine and human soluble epoxide hydrolase inhibition by urea-like compounds
A data set of 348 urea-like compounds that inhibit the soluble epoxide hydrolase enzyme in mice and humans is examined. Compounds having IC50 values ranging from 0.06 to >500 μM (murine) and 0.10 to >500 μM (human) are categorized as active or
McElroy, Nathan R.,Jurs, Peter C.,Morisseau, Christophe,Hammock, Bruce D.
p. 1066 - 1080
(2003)
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Chemistry of phosphorus ylides: Part 45 synthesis of phosphoranylidene, thietane, azetidine and thiazinane derivatives as potent chemo preventative agents
Reactions of nucleophilic active phosphacumulenes with iso(thio)cyanate compounds were performed. The reaction products depend on the nature of the reagent, substrate and the condition of the reaction used. New heterocyclic 4-membered or 6-membered sulfur
Hashem, Ahmed I.,El-Hussieny, Marwa,Abd-El-Maksoud, Mansoura A.,Maigali, Soher S.,Mansour, Shaimaa T.,Soliman, Fouad M.
p. 1 - 9
(2017/09/25)

N,N′-diarylurea compounds and N,N′-diarylthiourea compounds as inhibitors of translation initiation
Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.
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(2016/09/26)

ACTIVATORS OF MYOSIN II FOR MODULATING CELL MECHANICS
The present invention discloses small molecule compounds as activators of myosin II by promoting its assembly and recruitment to contractile structures in the cell and methods of using such compounds. These compounds are useful to modulate cell and tissue mechanics. This class of molecules, which affect cell mechanics either by activating the contractile system of the cell or modulating cytokinesis, will be used for therapeutic and tissue engineering applications.
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(2015/07/07)

A simple and efficient synthesis of diaryl ureas with reduction of the intermediate isocyanate by triethylamine
Thirty symmetrical diaryl urea derivatives were synthesised in moderate to excellent yields from arylamine and triphosgene with triethylamine as a reducing agent for the intermediate, isocyanate. It was significant that part of the products could be collected in almost quantitative yield without column chromatography. The procedure under mild reaction conditions was tolerant of a wide range of functional groups. The structures of the compounds were determined by NMR, MS and X-ray crystallographic analyses.
Zhou, Shuguang,Yao, Ting,Yi, Jicheng,Li, Dashuai,Xiong, Jing
p. 315 - 319
(2013/07/27)

In vitro inhibition of translation initiation by N,N′-diarylureas - Potential anti-cancer agents
Symmetrical N,N′-diarylureas: 1,3-bis(3,4-dichlorophenyl)-, 1,3-bis[4-chloro-3-(trifluoromethyl)phenyl]- and 1,3-bis[3,5- bis(trifluoromethyl)phenyl]urea, were identified as potent activators of the eIF2α kinase heme regulated inhibitor. They reduce the abundance of the eIF2·GTP·tRNAiMet ternary complex and inhibit cancer cell proliferation. An optimization process was undertaken to improve their solubility while preserving their biological activity. Non-symmetrical hybrid ureas were generated by combining one of the hydrophobic phenyl moieties present in the symmetrical ureas with the polar 3-hydroxy-tolyl moiety. O-alkylation of the later added potentially solubilizing charge bearing groups. The new non-symmetrical N,N′-diarylureas were characterized by ternary complex reporter gene and cell proliferation assays, demonstrating good bioactivities. A representative sample of these compounds potently induced phosphorylation of eIF2α and expression of CHOP at the protein and mRNA levels. These inhibitors of translation initiation may become leads for the development of potent, non-toxic, and target specific anti-cancer agents.
Denoyelle, Séverine,Chen, Ting,Chen, Limo,Wang, Yibo,Klosi, Edvin,Halperin, José A.,Aktas, Bertal H.,Chorev, Michael
supporting information; experimental part
p. 402 - 409
(2012/02/04)

Carbonic anhydrase inhibitors - Part 49: Synthesis of substituted ureido and thioureido derivatives of aromatic/heterocyclic sulfonamides with increased affinities for isozyme I
Reaction of nine aromatic/heterocyclic sulfonamides containing a free amino group with aryl isocyanates/isothiocyanates or allyl isothiocyanate afforded the corresponding urea/thiourea derivatives, which were characterized by standard physico-chemical procedures and assayed as inhibitors of three isozymes of carbonic anhydrase (CA), i.e. hCA I, hCA II and bCA IV (h = human, b = bovine isozyme). Another series of compounds, 1,5-disubstituted-2-thiobiuret derivatives, were prepared by reaction of 3,4-dichlorophenyl isocyanate with thioureido-containing aromatic/heterocyclic sulfonamides. Good inhibition of all these three CA isozymes was observed with the new compounds, but an exciting finding was that the ureas/thioureas and especially the above-mentioned thiobiurets reported here have an increased affinity to the slow isozyme hCA I, generally less susceptible to inhibition by sulfonamides, as compared to the rapid isozymes hCA II and bCA IV. Some of the new compounds might constitute good lead molecules for developing more selective CA I inhibitors.
Supuran, Claudiu T.,Scozzafava, Andrea,Jurca, Bogdan C.,Ilies, Marc A.
p. 83 - 93
(2007/10/03)

SUBSTITUENT EFFECTS ON HYDROLYTIC STABILITY AND HERBICIDAL ACTIVITY OF 3-ARYLIMIDAZOLIDINE-2,4-DIONES
Twenty-one derivatives of imidazolidine-2,4-dione have been prepared by reactions of substituted amino acids with aryl isocyanates in aqueous medium.Pre- and post-emergent herbicidal activities of all the compounds have been tested, and stability of five derivatives has been followed in aqueous medium within the pH range from 7.6 to 13.0.The highest pre-emergent herbicidal activity has been found with the derivatives XI-XVI which inhibit the growth of most indicator plants at the doses of 1.6 kg/ha.The derivatives studied are relatively stable in aqueous medium, the hydrolysis half-life of the compound XI being 9 days at pH 8.
Cegan, Alexandr,Vecera, Miroslav
p. 1521 - 1528
(2007/10/02)

THERMAL DECOMPOSITION OF SUBSTITUTED UREAS
The thermal dissociation of N,N'-diaryl- and N,N-dimethyl-N'-aryl-ureas was investigated under isothermal conditions in absence of solvent.In the case of N,N-dimethyl-N'-arylureas enthalpies of reaction were determined, and their relation to Hammett ? constants was shown.
Chimishkyan, A. L.,Svetlova, L. P.,Leonova, T. V.,Gluyaev, N. D.
p. 1317 - 1320
(2007/10/02)