- LIGAND-DIRECTED COVALENT MODIFICATION OF PROTEIN
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The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.
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Page/Page column
(2013/03/26)
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- 1,2-H shift in copper-chlorocarbenoid intermediate during CuCl/bpy-promoted stereoselective dechlorination of 2,2,2-trichloroethyl alkyl ethers to (Z)-1-alkoxy-2-chloroethenes
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(Chemical Equation Presented) Reaction of 2,2,2-trichloroethyl alkyl ethers with 2 molar equiv of CuCl/bpy in refluxing DCE yielded (Z)-1-alkoxy-2- chloroethenes stereoselectively as the major product via 1,2-H shift in copper-chlorocarbenoid intermediate. 2,2,2-Trichloroethyl carboxylates undergo a radical 1,2-acyloxy shift under similar conditions.
- Ram, Ram N.,Manoj
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supporting information; experimental part
p. 2243 - 2246
(2009/05/11)
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- Physical, chemical, and isotopic (atomic) labels
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Chemical or isotopic labels are added to, e.g., a potentially lethal drug formulation, to generate a unique chemical fingerprint. Combinations of chemical additives are mixed with the drug to aid in their isolation and identification, especially when such drugs are used for illicit purposes. When stable isotopes are incorporated into lethal drugs, the labeling process conveys a very unique internal chemical signature and greatly aids in the identification of the parent drug in body fluids and tissues. When heath-care providers become aware that certain drugs can now be easily tracked and identified in a victim, individuals may be reluctant to utilize these agents for ill purposes.
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- Hapten Synthesis and Production of Monoclonal Antibodies to DDT and Related Compounds
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This work describes the production and characterization of monoclonal antibodies (MAbs) to the organochlorine insecticide DDT and their incorporation into several ELISA configurations. A collection of DDT haptens was synthesized by introducing appropriate spacers at two sites of the analyte molecular structure. From mice immunized with hapten-protein conjugates, MAbs with I50 values to p,p'-DDT in the 2-11 nM range in homologous conjugate-coated assays were obtained. According to their cross-reactivity pattern with DDT isomers and metabolites, MAbs can be classified as class-specific or DDT-specific antibodies. Both types of MAbs were obtained from mice immunized with the same hapten-protein conjugate simply by applying a different selection criterion in the screening of fusion supernatants. These immunoassays are potentially very valuable analytical tools for the rapid and sensitive determination of DDT and congeners in food and the environment and for monitoring human exposure to these ubiquitous and toxic compounds.
- Abad, Antonio,Manclus, Juan J.,Mojarrad, Fatemeh,Mercader, Josep V.,Miranda, Miguel A.,Primo, Jaime,Guardiola, Vicente,Montoya, Angel
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p. 3694 - 3702
(2007/10/03)
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- Process for the preparation of 1,1-bis(4-chlorophenyl)-2,2,2-trichloroethanol
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1,1-bis(4-chlorophenyl)-2,2,2-trichloroethanol is separated from a mixture comprising by way of the formation of an addition compound between 1,1-bis(4-chlorophenyl)-2,2,2-trichloroethanol and a moderately electron donating compound, preferably selected from a group formed by dimethyl sulphoxide, cyclohexanone, isophoron, pyridine, 1,4-dioxane, acetic acid, acetonitrile and water.
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- Process for preparing environmentally safe dicofol and its formulations
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The present invention provides for an improved practical process for producing DDTr-free p,p'-dicofol and its formulations substantially free of the practically inactive o-p'-dicofol comprising either directly recrystallizing technical dicofol from a suitable solvent such as acetic acid or alkanes, or alternatively preparing the p,p'-dicofol by the steps of (a) dehydrohalogenating technical DDT to give DDE; (b) chlorinating DDE to give Cl-DDT; and (c) hydrolyzing Cl-DDT to dicofol, wherein the technical DDT is initially recrystallized from a suitable solvent such as lower alkyl alcohols and then recrystallizing the ressulting p,p'-dicofol from a suitable solvent such as acetic acid or alkanes.
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- Ammonium stannates-(IV)
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Ammonium stannates of the formula in which the symbols R1, R2, R3, R4, R7, X, Y, a, b, c, d, n, q, r, t and w are as defined in the description, are effective biocides. They can be used both for the protection of materials and for protecting crop plants. Their good solubility in water and their low volatility are particularly valuable properties.
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- Alkyl 4-[o-(substituted methyleneamino)phenyl]-3-thioallophanates
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Various alkyl 4-[o-(substituted methyleneamino)phenyl] 3-thioallophanates are useful as fungicides and mite ovicides. The compounds are prepared by reacting alkyl 4-(o-aminophenyl)-3-thioallophanates with aldehydes or trialkyl orthoformates. Some of the compounds are prepared by further reacting the reaction product of an alkyl 4-(o-aminophenyl)-3-thioallophanate and a trialkyl orthoformate with a primary or secondary amine. Exemplary species are methyl 4-[o-(o-fluorobenzylideneamino)phenyl]-3-thioallophanate, methyl 4-[o-(4-methylbenzylideneamino)phenyl]-3-thioallophanate and methyl 4-[o-(2-furfurylideneamino)phenyl]-3-thioallophanate.
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- Alkyl 4-[o-(substituted methyleneamino)-phenyl]-3-thioallophanate miticides and fungicides
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Various alkyl 4-[o-(substituted methyleneamino)phenyl]3-thioallophanates are useful as fungicides and mite ovicides. The compounds are prepared by reacting alkyl 4-(o-aminophenyl)-3-thioallophanates with aldehydes or trialkyl orthoformates. Some of the compounds are prepared by further reacting the reaction product of an alkyl 4-(o-aminophenyl)-3-thioallophanate and a trialkyl orthoformate with a primary or secondary amine. Exemplary species are methyl 4-[o-(o-fluorobenzylideneamino)phenyl]-3-thioallophanate, methyl 4-[o-(4-methylbenzylideneamino)phenyl]-3-thioallophanate and methyl 4-[o-(2-furfurylideneamino)phenyl]-3-thioallophanate.
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- Propynyl benzyl ethers
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Propynyl benzyl ethers having juvenile hormone-like activity which are 4-halogen, lower alkyl, lower alkoxy or propynyloxy substituted or 3,4-lower alkylenedioxy substituted and which can also be 3,5- and/or α-substituted, and insecticide compositions that include at least one propynyl benzyl ether and that can also include a conventional insect-poison.
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- Alkyl 4-(o-aminophenyl)-3-thioallophanates
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Various alkyl 4-(o-aminophenyl)-3-thioallophanates and alkyl 4-(o-alkylaminophenyl)-3-thioallophanates are useful as fungicides and mite ovicides. The compounds are prepared by reacting an o-phenylenediamine with the appropriate alkoxycarbonylisothiocyanate and an exemplary species is methyl 4-(o-aminophenyl)-3-thioallophanate.
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- Pesticidal alkyl 4-(0-(substituted methyleneamine)-phenyl)-3-thioallophanates
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Various alkyl 4-[o-(substituted methyleneamino)phenyl] 3-thioallophanates are useful as fungicides and mite ovicides. The compounds are prepared by reacting alkyl 4-(o-aminophenyl)-3-thioallophanates with aldehydes or trialkyl orthoformates. Some of the compounds are prepared by further reacting the reaction product of an alkyl 4-(o-aminophenyl)-3-thioallophanate and a trialkyl orthoformate with a primary or secondary amine. Exemplary species are methyl 4-[o-(o-fluorobenzylidine-amino)phenyl]-3-thioallophanate, methyl 4-[o-(4-methylbenzyl-ideneamino)phenyl]-3-thioallophanate and methyl 4-[o-(2-furfuryl-ideneamino)phenyl]-3-thioallophanate.
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