- 3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1
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Investigation of 1N-substituted pyrazole-3-carboxanilides as 15-lipoxygenase-1 (15-LOX-1) inhibitors demonstrated that the 1N-substituent was not essential for activity or selectivity. Additional halogen substituents on the pyrazole ring, however, increased activity. Further development led to triazole-4-carboxanilides and 2-(3-pyrazolyl) benzoxazoles, which are potent and selective 15-LOX-1 inhibitors.
- Pelcman, Benjamin,Sanin, Andrei,Nilsson, Peter,No, Kiyo,Schaal, Wesley,?hrman, Sara,Krog-Jensen, Christian,Forsell, Pontus,Hallberg, Anders,Larhed, Mats,Boesen, Thomas,Kromann, Hasse,Vogensen, Stine Byskov,Groth, Thomas,Claesson, Hans-Erik
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p. 3024 - 3029
(2015/06/22)
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- Substituted piperazines
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Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
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- 1-ARYL-4-SUBSTITUTED PIPERAZINES DERIVATIVES FOR USE AS CCR1 ANTAGONISTS FOR THE TREATMENT OF INFLAMMATION AND IMMUNE DISORDERS
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Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
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- Use of low-volatility pyrazole derivatives having hydrophilic groups as nitrification inhibitors
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The present invention provides pyrazole compounds which are useful as nitrification inhibitors.
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- Enzymatic Halogenation of Pyrazoles and Pyridine Derivatives
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Pyrazole, 1-methylpyrazole and 3-methylpyrazole are chlorinated by the enzyme chloroperoxidase from Caldariomyces fumago, in the presence of potassium chloride and hydrogen peroxide at pH 2.7, yielding the corresponding 4-chloro derivatives in good yields.A 4H-pyrazole is proposed as an intermediate in this reaction. 2-Aminopyridine was converted regiospecifically by the same enzyme into 2-amino-3-chloropyridine, and 8-hydroxyquinoline gave its 5,7-dibromo-derivatives in very good yield when bromide ion was used as halide substrate.
- Franssen, M. C. R.,van Boven, H. G.,van der Plas, H. C.
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p. 1313 - 1316
(2007/10/02)
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