126076-76-4Relevant articles and documents
ARYL-SULFONAMIDE AND ARYL-SULFONE DERIVATIVES AS TRPML MODULATORS
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Page/Page column 57, (2018/12/03)
The new arylsulfonamide and arylsulfone derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities and lysosome functions such as acid-related disorders and cancer.
A practical in situ generation of the schwartz reagent. reduction of tertiary amides to aldehydes and hydrozirconation
Zhao, Yigang,Snieckus, Victor
, p. 390 - 393 (2014/04/03)
A new, highly efficient in situ protocol (Cp2ZrCl2/LiAlH(OBu-t)3) is described for the generation of the Schwartz reagent which provides a convenient method for the amide to aldehyde reduction and the regioselective hydrozirconation-iodination of alkynes and alkenes. Highlighted are chemoselective reductions of benzamides derived by directed ortho metalation (DoM) chemistry, allowing the synthesis of valuable 1,2,3-substituted benzaldehydes. The single-step, three-component process proceeds in a very short reaction time, shows excellent functional group compatibility, and uses inexpensive and long-storage stable reducing reagents.
2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists
Andrés, Miriam,Bravo, Mónica,Buil, Maria Antonia,Calbet, Marta,Castillo, Marcos,Castro, Jordi,Eichhorn, Peter,Ferrer, Manel,Lehner, Martin D.,Moreno, Imma,Roberts, Richard S.,Sevilla, Sara
, p. 168 - 184 (2014/01/06)
In this manuscript, the synthesis and biological activity of a series of pyrazole acetic acid derivatives as CRTh2 antagonists is presented. Biological evaluation in vitro revealed that the pyrazole core showed in several cases a different structure-activity relationship (SAR) to that of related indole acetic acid. A potent series of ortho-sulfonyl benzyl substituents was found, from which compounds 27 and 63 were advanced to in vivo profiling.