138907-73-0Relevant articles and documents
Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
Dos Santos, Maurício Silva,Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo
, p. 335 - 343 (2021/09/07)
Hybrid systems containing pyrazole moiety show a wide spectrum of biological activities. To access novel hybrids with pyrazole ring, in this work we synthesized twenty pyrazole-carboxylic acids and twenty pyrazole-carboxamides, using simple synthetic methods, to be used as building blocks in the development of new structures.
Cu-promoted sydnone cycloadditions of alkynes: Scope and mechanism studies
Comas-Barcel?3, Jffllia,Foster, Robert S.,Fiser, B??la,Gomez-Bengoa, Enrique,Harrity, Joseph P. A.
supporting information, p. 3257 - 3263 (2015/03/05)
Cu salts have been found to promote the cycloaddition reaction of sydnones and terminal alkynes, providing significant reduction in reaction times. Specifically, the use of Cu(OTf)2 is found to provide 1,3-disubstituted pyrazoles, whereas simpl
nBu3P-catalyzed desulfonylative [3 + 2] cycloadditions of allylic carbonates with arylazosulfones to pyrazole derivatives
Zhang, Qi,Meng, Ling-Guo,Wang, Kuai,Wang, Lei
supporting information, p. 872 - 875 (2015/04/21)
Highly efficient nBu3P-catalyzed desulfonylative [3 + 2] cycloadditions of allylic carbonates with arylazosulfones were developed for the synthesis of pyrazole derivatives. The reactions proceed smoothly under mild conditions to gene
Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains
Sutherland, Hamish S.,Blaser, Adrian,Kmentova, Iveta,Franzblau, Scott G.,Wan, Baojie,Wang, Yuehong,Ma, Zhenkun,Palmer, Brian D.,Denny, William A.,Thompson, Andrew M.
supporting information; experimental part, p. 855 - 866 (2010/06/15)
Recently described biphenyl analogues of the antituberculosis drug PA-824 displayed improved potencies against M. tuberculosis but were poorly soluble. Heterobiaryl analogues of these, in which the first phenyl ring was replaced with various 5-membered ring heterocycles, were prepared with the aim of identifying potent new candidates with improved aqueous solubility. The compounds were constructed by coupling the chiral 2-nitroimidazooxazine alcohol with various halomethyl-substituted arylheterocycles, by cycloadditions to a propargyl ether derivative of this alcohol, or by Suzuki couplings on haloheterocyclic methyl ether derivatives. The arylheterocyclic compounds were all more hydrophilic than their corresponding biphenyl analogues, and several showed solubility improvements. 1-Methylpyrazole, 1,3-linked-pyrazole, 2,4-linked-triazole, and tetrazole analogues had 3- to 7-fold higher MIC potencies against replicating M. tb than predicted by their lipophilicities. Two pyrazole analogues were >10-fold more efficacious than the parent drug in a mouse model of acute M. tb infection, and one displayed a 2-fold higher solubility. 2009 American Chemical Society.
PYRAZOLE DERIVATIVES AS P2X7 MODULATORS
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Page/Page column 65, (2009/01/20)
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The pyrazole derivatives of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2
AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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Page 46, (2010/01/31)
The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
3-(1-SUBSTITUTED-PYRAZOYL)-2-OXINDOLE DERIVATIVES, COMPOSITIONS AND USE
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, (2008/06/13)
This invention relates to novel 3-(1-substituted-pyrazoyl)-2-oxindole derivatives which are inhibitors of prostaglandin H2 synthease, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H