5930-92-7Relevant articles and documents
Synthesis and X-ray structure of stable 2H-isoindoles
Murashima, Takashi,Tamai, Ryuji,Nishi, Keiji,Nomura, Kentaroh,Fujita, Ken-Ichi,Uno, Hidemitsu,Ono, Noboru
, p. 995 - 998 (2000)
Stable 2H-isoindoles with electron-withdrawing groups were prepared using the reaction of dinitrobenzene derivatives with isocyanoacetate in the presence of DBU. The use of acetonitrile as the solvent or a phosphazene base (BTPP) as a non-ionic base improved the yields. The structure was confirmed by X-ray crystallographic analysis of the compound 2e′. According to the X-ray analysis, this substance existed in the solid phase only as the 2H-isomer. The Royal Society of Chemistry 2000.
New synthetic equivalent of nitromalonaldehyde treatable in organic media
Nishiwaki, Nagatoshi,Ogihara, Takuma,Takami, Toshiko,Tamura, Mina,Ariga, Masahiro
, p. 8382 - 8386 (2007/10/03)
β-Nitroenamines having a formyl group at the β-position behave as the synthetic equivalent of unstable nitromalonaldehyde, which is a useful synthon for syntheses of versatile nitro compounds. High solubility of the nitroenamines into general organic solv
3-PYRROLYL UREA DERIVATIVES AND THEIR USE AS ANTIVIRAL AGENTS
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Page 31-32, (2010/02/07)
The invention relates to substituted pyrroles of formula (I), in which: R1 represents -OR8 or -NR9R10; R2 represents hydrogen, C1-C6 alkyl or aryl, whereby R2 as an alkyl can be substituted with 0, 1, 2 or 3 substituents R2-1 independently of one another, selected from the group comprising halogen, hydroxy, C1-C6 alkoxy, hydroxycarbonyl, C1-C6 alkoxycarbonyl, C1-C6alkylcarbonyloxy, amino, C1-C6 alkylamino, aminocarbonyl, C1-C6 alkylaminocarbonyl, C3-C8 cycloalkyl, a 5- to 10-membered heterocyclyl, C6-C10 aryl, phenoxy and a 5- to 10-membered heteroaryl and whereby R2 as an aryl can be substituted with 0, 1, 2 or 3 substituents R2-2 independently of one another, selected from the group comprising halogen, hydroxy, nitro, cyano, trifluoromethyl, trifluoromethoxy, C1-C6 alkyl, C1-C6 alkoxy, hydroxycarbonyl, C1-C6 alkoxycarbonyl, amino, C1-C6 alkylamino, aminocarbonyl, C1-C6 alkylaminocarbonyl, C3-C8 cycloalkyl, a 5- to 10-membered heterocyclyl, C6-C10 aryl and a 5- to 10-membered heteroaryl; R3 and R4 independently of one another represent hydrogen or C1-C6 alkyl; R5 and R6 independently of one another represent hydrogen or C1-C6 alkyl; and R7 represents a 3- to 12-membered carbocyclyl, whereby the carbocyclyl can be substituted with 0, 1, 2, 3, 4 or 5 substituents independently of one another, selected from the group comprising halogen, hydroxy, C1-C6 alkyl and C1-C6 alkoxy. The invention also relates to a method for producing said pyrroles, to their use for the treatment and/or prophylaxis of diseases, in addition to their use for producing medicaments for the treatment and/or prophylaxis of diseases, notably to their use as antiviral agents, in particular against cytomegaloviruses.
Halogen-substitued thienyl compounds
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, (2008/06/13)
Halogen substituted thienyl compounds exhibit potential as nucleic acid (especially double stranded DNA) binders and as antibiotic compounds. A representative thienyl compound has the structure
Recognition of the DNA minor groove by pyrrole-imidazole polyamides: Comparison of desmethyl- and N-methylpyrrole
Bremer, Ryan E.,Szewczyk, Jason W.,Baird, Eldon E.,Dervan, Peter B.
, p. 1947 - 1955 (2007/10/03)
Polyamides consisting of N-methylpyrrole (Py), N-methylimidazole (Im), and N-methyl-3-hydroxypyrrole (Hp) are synthetic ligands that recognize predetermined DNA sequences with affinities and specificities comparable to many DNA-binding proteins. As derivatives of the natural products distamycin and netropsin, Py/Im/Hp polyamides have retained the N-methyl substituent, although structural studies of polyamide:DNA complexes have not revealed an obvious function for the N-methyl. In order to assess the role of the N-methyl moiety in polyamide:DNA recognition, a new monomer, desmethylpyrrole (Ds), where the N-methyl moiety has been replaced with hydrogen, was incorporated into an eight-ring hairpin polyamide by solid-phase synthesis. MPE footprinting, affinity cleavage, and quantitative DNase I footprinting revealed that replacement of each Py residue with Ds resulted in identical binding site size and orientation and similar binding affinity for the six-base-pair (bp) target DNA sequence. Remarkably, the Ds-containing polyamide exhibited an 8-fold loss in specificity for the match site versus a mismatched DNA site, relative to the all-Py parent. Polyamides with Ds exhibit increased water solubility, which may alter the cell membrane permeability properties of the polyamide. The addition of Ds to the repertoire of available monomers may prove useful as polyamides are applied to gene regulation in vivo. However, the benefits of Ds incorporation must be balanced with a potential loss in specificity. Copyright (C) 2000 Elsevier Science Ltd.
