- 1 -HYDROXY-BENZOOXABOROLES AS ANTIPARASITIC AGENTS
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Provided are compounds useful for controlling endoparasites both in animals and agriculture. Further provided are methods for controlling endoparasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling endoparasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. The claimed compounds are described by the following Markush formula:A typical example for a compound according to above formula is: A typical example for a compound according to above formula is:
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Page/Page column 74
(2014/10/03)
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- TRISUBSTITUTED BORON-CONTAINING MOLECULES
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This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.
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Page/Page column 113
(2011/02/24)
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- Sulfur-substituted α-alkyl phenethylamines as selective and reversible MAO-A inhibitors: Biological activities, CoMFA analysis, and active site modeling
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A series of phenethylamine derivatives with various ring substituents and with or without N-methyl and/or C-α methyl or ethyl groups was synthesized and assayed for their ability reversibly to inhibit monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). Several compounds showed potent and selective MAO-A inhibitory activity (IC50 in the submicromolar range) but none showed appreciable activity toward MAO-B. A three-dimensional quantitative structure-activity relationship study for MAO-A inhibition was performed on the series using comparative molecular field analysis (CoMFA). The resulting model gave a cross-validated q2 of 0.72 and showed that in this series of compounds steric properties of the substituents were more important than electrostatic effects. Molecular modeling based on the recently published crystal structure of inhibitor-bound MAO-A provided detailed evidence for specific interactions of the ligands with the enzyme, supported by previous references and consistent with results from the CoMFA. On the basis of these results, structural determinants for selectivity of substituted amphetamines for MAO-A are discussed.
- Gallardo-Godoy, Alejandra,Fierro, Angélica,McLean, Thomas H.,Castillo, Mariano,Cassels, Bruce K.,Reyes-Parada, Miguel,Nichols, David E.
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p. 2407 - 2419
(2007/10/03)
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- Reaction of Some 1,4-Benzoquinone Mono-oximes with Methanolic Hydrogen Chloride
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When 2-methyl-1,4-benzoquinone 4-oxime (1) reacted with methanolic hydrogen chloride at 25-30 deg C the product was 2-chloro-4,6-dimethoxy-3-methylaniline (2).Similarly 1,4-benzoquinone 4-oxime (7) gave 2-chloro-4,6-dimethoxyaniline (8), 3-methyl-1,4-benzoquinone 4-oxime (11) gave 2-chloro-4-methoxy-6-methoxymethylaniline (12) and 2-chloro-4-methoxy-6-methylaniline (13), and 2-methoxy-1,4-benzoquinone 4-oxime (19) gave 2-chloro-4,5-dimethoxyaniline (20).
- Sargent, Melvyn V.
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p. 1095 - 1098
(2007/10/02)
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