24115-20-6Relevant articles and documents
Synthesis of aryloxyacetonitriles based on arylboronic acids with 2-bromoacetonitrile
Li, Yingmin,Guo, Mengping,Wen, Yongju,Zhou, Lanjiang,Shen, Xiuli,Kang, Yangping
supporting information, (2020/09/09)
A new and efficient protocol for the synthesis of aryloxyacetonitriles based on arylboronic acids with 2-bromoacetonitrile has been developed using eco-friendly hydrogen peroxide as oxidant under metal-free conditions. This method is compatible with arylboronic acid attached sensitive substituent and obtains desired product in moderate to good yield.
Combinatorial synthesis and in vitro evaluation of a biaryl hydroxyketone library as antivirulence agents against mrsa
Yu, Guanping,Kuo, David,Shoham, Menachem,Viswanathan, Rajesh
supporting information, p. 85 - 91 (2014/03/21)
Antibiotic resistance coupled with decreased development of new antibiotics necessitates the search for novel antibacterial agents. Antivirulence agents offer an alternative to conventional antibiotics. In this work, we report on a family of small-molecule antivirulence agents against methicillin-resistant Staphylococcus aureus (MRSA), the most widespread bacterial pathogen. Structure-activity relationship studies led to the development of a concise synthesis of a 148-member biarylhydroxyketone library. An acylation bond-forming process afforded resorcinols (1) and aryloxy acetonitriles (2) as synthons. A Lewis-acid-activated Friedel-Crafts' acylation step involving a nitrile functionality of 2 by ZnCl2, followed by nucleophilic attack by 1 was executed to obtain biaryl hydroxyketones in excellent yields. A large number of products crystallized. This strategy affords a range of biarylhydroxyketones in a single step. This is the first collective synthetic study documenting access to this class of compounds through a single synthetic operation. In vitro efficacy of compounds in this library was evaluated by a rabbit erythrocyte hemolysis assay. The most efficacious compound, 4f-12, inhibits hemolysis by 98.1 ± 0.1% compared to control in the absence of the compound.
Imidazo-substituted compounds as p38 kinase inhibitors
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Page 18, (2008/06/13)
The present invention discloses compounds corresponding to formula I: wherein A, Z, Z1, Y, R1 and R2 are as defined in the specification, as well as pharmaceutical formulations, methods of making and uses thereof.