- γ-cui nanocrystals from self-assembled coordination polymers
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Step by step: Two stairstep Cu4I4 coordination polymers 1 and 2 have selectively been synthesized by self-assembly of CuI and 1,4-bis(2-methylthioethoxy)benzene. γ-Cul nanocrystals have been prepared by thermal decomposition of the two stairstep Cu4I4 coordination polymers. Crystal transformation from the two polymers to a cubane Cu4I4 coordination polymer 3 has been observed at initial stage of γ-Cul nanocrystal preparation.
- Kim, Tae Ho,Yang, Hojin,Park, Garam,Lee, Kang Yeol,Kim, Jineun
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- O2-sulfonylethyl protected isopropylamine diazen-1-ium-1,2- diolates as nitroxyl (HNO) donors: Synthesis, β-elimination fragmentation, HNO release, positive inotropic properties, and blood pressure lowering studies
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New types of nonexplosive O2-sulfonylethyl protected (-CH 2CH2SO2R; R = OMe, NHOMe, NHOBn, Me) derivatives of isopropylamine diazen-1-ium-1,2-diolate (IPA/NO) (2-5) were developed that are designed to act as novel HNO donors. These compounds, with suitable half-lives (6.6-17.1 h) at pH 7.4, undergo a base-induced β-elimination reaction that releases a methyl vinyl sulfone product and the parent IPA/NO anion which subsequently preferentially releases HNO (46-61% range). Importantly, the O2-methylsulfonylethyl compound 5 exhibited a significant in vitro inotropic effect up to 283% of the baseline value and increased the rates of contraction and relaxation but did not induce a chronotropic effect. Furthermore, compound 5 (22.5 mg/kg po dose) provided a significant reduction in blood pressure up to 6 h after drug administration. All these data suggest that O2-sulfonylethyl protected derivatives of IPA/NO, which are efficient HNO donors, could have potential applications to treat cardiovascular disease(s) such as congestive heart failure.
- Huang, Zhangjian,Kaur, Jatinder,Bhardwaj, Atul,Alsaleh, Nasser,Reisz, Julie A.,DuMond, Jenna F.,King, S. Bruce,Seubert, John M.,Zhang, Yihua,Knaus, Edward E.
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supporting information
p. 10262 - 10271
(2013/01/16)
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- Heterocyclic substituted 2-methyl-benzimidazole antiviral agents
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The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.
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- Synthesis and Binding Affinities of Novel Re-Containing 7α-Substituted Estradiol Complexes: Models for Breast Cancer Imaging Agents
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The diagnosis and staging of breast cancer could be improved by the development of imaging radiopharmaceuticals that provide a noninvasive determination of the estrogen receptor status in the tumor cells. Toward this goal, we have synthesized a number of novel Re-containing 7α-substituted estradiol complexes. The introduction of the 7α side chain involves the alkylation of tetrahydropyranyloxy-protected 6-keto estradiol. The methods used to introduce the rhenium metal involve "3 + 1" and "4 + 1" mixed ligand complexes (2a-c and 5, respectively), tricarbonyl dithioether complexes (3), and the cyclopentadienyltricarbonylmetal organometallic system (4ab, 6, 7). These complexes showed binding affinities for the estrogen receptor (as high as 45% for the "3 + 1" complex 2c) when compared to the native ligand estradiol. The polarity of some complexes (4ab) was modified to improve biodistribution properties by introducing (poly)ether linkages into the 7α side chain (6, 7). These complexes provide a further refinement of our understanding of ligand structure-binding affinity correlations for the estrogen receptor, and they furnish the synthetic groundwork for the synthesis of the analogous Tc-99m complexes for evaluation as breast tumor imaging agents.
- Skaddan, Marc B.,Wuest, Frank R.,Katzenellenbogen, John A.
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p. 8108 - 8121
(2007/10/03)
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- Synthesis of rhenium(I) and technetium(I) carbonyl/dithioether ligand complexes bearing 3,17β-estradiol
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Tricarbonyldithioethermetal(I) complexes of rhenium and technetium with a pendant 3,17β-estradiol have been synthesized and characterized. The steroid ligand was bound to the metal centre by the two sulfur atoms of a 4,7-dithiaoct-1-ine spacer.
- Reisgys, Martina,Wuest, Frank,Alberto, Roger,Schibli, Roger,Schubiger, Paul August,Pietzsch, Hans-Juergen,Spies, Hartmut,Johannsen, Bernd
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p. 2243 - 2246
(2007/10/03)
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- Reaction Mechanism of Cathodic Crossed Coupling of Acetone with Unsaturated Compounds in Acidic Solution
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It was confirmed that the cathodic crossed coupling of acetone with unsaturated compounds in aqueous sulfuric acid could proceed smoothly, when the compounds which had radical-acceptable double bonds and were adsorbed on a mercury cathode were used.From this fact, it was concluded that the coupling occurs via the addition of a radical intermediate formed by the one-electron reduction of acetone to the double bonds on the cathode surface.Possibility of the addition of an anionic intermediate derived from acetone was excluded by no occurrence of the coupling of acetone with a polar acetylenic triple bond compound adsorbed on the cathode.
- Koizumi, Toshio,Fuchigami, Toshio,Kandeel, Zaghloul El-Shahat,Sato, Norio,Nonaka, Tsutomu
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p. 757 - 762
(2007/10/02)
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- THE CONVERSION OF 2-(METHYLTHIO)ETHANOL INTO 1-CHLORO-2-(METHYLTHIO)-ETHANE: A 13C-LABELLING STUDY WITH THE AID OF 13C NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY
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The synthesis of 2-(methylthio)ethanol from acetic acid is described.This labelled alcohol and 13C NMR spectrocopy were used to evaluate the propensity for rearrangement of four methods for effecting the conversion ROH RCl.In every case the product observed at all stages of the reaction was a 1:1 mixture of 1-chloro-2-(methylthio)ethane and 1-chloro-2-(methylthio)ethane.It is proposed that activation of the hydroxy-group of 2-(methylthio)ethanol is followed by internal displacement by the methylthio-group giving the 1-methylthiiranium ion, which is captured by chloride.
- Billington, David C.,Golding, Bernard T.
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p. 341 - 348
(2007/10/02)
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- The chemistry of methyltitanium trichloride. II. Variable-temperature nuclear magnetic resonance and infrared spectra of some complexes of methyltitanium trichloride and of titanium tetrachloride with unsymmetrical bidentate ligands
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The pseudooctahedral complexes of methyltitanium trichloride with the unsymmetrical bidentate ligands methyl β-dimethylaminoethyl ether, methyl β-methylthioethyl ether, and methyl β-dimethylaminoethyl sulfide are precipitated on mixing hexane solutions of methyltitanium trichloride and the appropriate ligand. They are intensely colored solids, extremely sensitive to atmospheric oxygen and moisture and thermally unstable, decomposing gradually on storage in vacuo at room temperature. The nmr spectra of the complexes show that, in solution, they prefer to adopt that meridional configuration in which the harder ligand atom lies trans to the titanium-methyl group. In their ir spectra, the complexes all show bands in the 450-490-cm-1 region, which are assigned to v(Ti-C). These bands are absent from the ir spectra of the corresponding complexes of titanium tetrachloride, which we have also prepared and characterized (mainly to assist in the assignment of nmr data). By contrast to the foregoing, the product isolated from the reaction of methyltitanium trichloride with N,N,N′,-N′-tetramethyl-o-aminobenzylamine (B) is a titanium(III) derivative which can be formulated as TiCl3 · B.
- Clark,McAlees
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p. 342 - 348
(2007/10/05)
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