- New and efficient synthesis of 3-arylquinazolin-4(1H)-ones and biologically important N-fused tetracycles based on N-(2-carboxyphenyl)oxalamide
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A novel clean, one-pot syntheses of 3-arylquinazolin-4(3H)-ones and quinoxalino[2,1-b]quinazoline-6,12(5H)-diones via PPA-mediated coupling of N-(2-carboxyphenyl)oxalamides with arylamines and 1,2-benzenediamines have been developed. Under mild reaction conditions with use of Na2S2O4 the benzimidazo[2,1-b]quinazolin-12-ones were achieved in good yield from 3-(2-nitrophenyl)quinazolin-4-ones.
- Mamedov, Vakhid A.,Mamedova, Vera L.,Syakaev, Victor V.,Gubaidullin, Aidar T.,Voronina, Julia K.,Kushatov, Temur A.,Korshin, Dmitry E.,Samigullina, Aida I.,Tanysheva, Ekaterina G.,Kh. Rizvanov, Il'dar,Latypov, Shamil K.
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- A novel acid-catalyzed rearrangement of 2-substituted-3-(2-nitrophenyl)oxiranes for the synthesis of di- and mono-oxalamides
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A novel one-pot synthetic approach to N1-(2-carboxyaryl)-N2-(aryl or H)oxalamides from 3-(2-nitroaryl)oxirane-2-carboxamides via the classical Meinwald rearrangement and a new rearrangement sequence has been developed. The methodology is applicable to the synthesis of N-(2-carboxyphenyl)aryloxalmonoamides from (3-(2-nitrophenyl)oxiran-2-yl)(aryl)methanones. The method is operationally simple and high yielding, thus providing a new useful formula for both anthranilic acid derivatives and oxalamides.
- Mamedov, Vakhid A.,Mamedova, Vera L.,Khikmatova, Gul'Nas Z.,Mironova, Ekaterina V.,Krivolapov, Dmitry B.,Bazanova, Olga B.,Chachkov, Denis V.,Katsyuba, Sergey A.,Rizvanov, Il'Dar Kh,Latypov, Shamil K.
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p. 27885 - 27895
(2016/03/30)
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- Synthesis, crystal structure, cytotoxicities and DNA-binding properties of a tetracopper(II) complex with N-benzoato-N0-[2-(2-hydroxyethylamino)ethyl- amino]oxamide ligand
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A new dissymmetrical N,N'-bis(substituted)- oxamide ligand, N-benzoato-N'-[2-(2- hydroxyethylamino)- ethyl]oxamide (H3bhyox), and its tetranuclear copper(II) complex, [Cu4(bhyox)2(dabt) 2](ClO4)2 (1) have been synthesized and characterized (dabt = 2,2'-diamino- 4,4'-bithiazole). The crystal structures of H3bhyox and complex 1 have been determined by X-ray single-crystal diffraction. Complex 1 has a cyclic tetranuclear cation with an embedded inversion center, in which the Cu-Cu separations through the oxamido and carboxyl bridges are 5.2246(6) and 5.3141(6) A , respectively. Both Cu(II) centers at the inner and outer sites of the cis-bhyox3- ligand have square pyramidal geometries. There is a 3D hydrogen-bonding network in the crystal. The cytotoxicities and DNA-binding properties of H3bhyox and complex 1 were studied. Both compounds can interact with HS- DNA by intercalation, and the DNA-binding affinities are consistent with their in vitro cytotoxicities. Springer Science+Business Media B.V. 2012.
- Chen, Wen-Cai,Wang, Ling-Dong,Li, Yan-Tuan,Wu, Zhi-Yong,Yan, Cui-Wei
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p. 569 - 577
(2012/11/13)
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- Modulators of protein tyrosine phosphatases (PTPases)
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The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, wherein A, R1, R2, R3, R4, R16and R17are as defined in the specification. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
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