On September 30, 2016, Diamanti, Eleonora; Bottegoni, Giovanni; Goldoni, Luca; Realini, Natalia; Pagliuca, Chiara; Bertozzi, Fabio; Piomelli, Daniele; Pizzirani, Daniela published an article.Application In Synthesis of 5-Methoxy-1H-pyrazole The title of the article was Pyrazole-Based Acid Ceramidase Inhibitors: Design, Synthesis, and Structure-Activity Relationships. And the article contained the following:
Acid ceramidase (a.c.) is a lysosomal cysteine amidase responsible for the cleavage of ceramide into sphingosine, which is then phosphorylated to sphingosine 1-phosphate. AC regulates the intracellular levels of ceramide and sphingosine, and a.c. inhibition may be useful in the treatment of disorders, such as cancer, in which ceramide-mediated signaling may be dysfunctional. Despite their potential exptl. and therapeutic value, the number of available small-mol. inhibitors of a.c. activity remains limited. In the present study is described the discovery of a class of potent pyrazole carboxamide-based a.c. inhibitors, which were identified using the at. property field (APF) approach and developed through systematic SAR studies and in vitro pharmacol. characterization. The best compound of this series inhibits a.c. with nanomolar potency and causes ceramide accumulation and sphingosine depletion in intact G361 proliferative melanoma cells. By expanding the current armamentarium of a.c. inhibitors, these results should facilitate future efforts to unravel the biol. of a.c. and the therapeutic potential of its inhibition. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Application In Synthesis of 5-Methoxy-1H-pyrazole
The Article related to alkyl isocyanate coupling reaction pyrazole, pyrazole carboxamide derivative preparation potent acid ceramidase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application In Synthesis of 5-Methoxy-1H-pyrazole
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics