- Synthesis of aryloxyacetonitriles based on arylboronic acids with 2-bromoacetonitrile
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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.
- Li, Yingmin,Guo, Mengping,Wen, Yongju,Zhou, Lanjiang,Shen, Xiuli,Kang, Yangping
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supporting information
(2020/09/09)
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- Combinatorial synthesis and in vitro evaluation of a biaryl hydroxyketone library as antivirulence agents against mrsa
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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.
- Yu, Guanping,Kuo, David,Shoham, Menachem,Viswanathan, Rajesh
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supporting information
p. 85 - 91
(2014/03/21)
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- SUBSTITUTED 2-INDOLINONE AS PTK INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to substituted 2-indolinone containing zinc- binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 54; 60
(2008/06/13)
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- MULTI-FUNCTIONAL SMALL MOLECULES AS ANTI-PROLIFERATIVE AGENTS
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The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.
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Page/Page column 204-205
(2008/06/13)
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- PHARMACEUTICAL PREPARATIONS COMPRISING INSULIN, ZINC IONS AND A ZINC-BINDING LIGAND
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Novel preparations comprising branched ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The preparations have a prolonged action designed for flexible injection regimes.
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Page/Page column 266
(2008/06/13)
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- PHAMACEUTICAL PREPARATIONS COMPRISING INSULIN
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Novel preparations comprising ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer wherein the ligand is extended by protamine that are capable of prolonging the ac-tion of insulin preparations.
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Page/Page column 261
(2010/02/15)
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- Stabilised insulin compositions
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The present invention provides pharmaceutical compositions comprising insulin and novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The resulting preparations have improved physical and chemical stability.
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Page/Page column 142
(2008/06/13)
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- Novel ligands for the hisb10 zn2+ sites of the r-state insulin hexamer
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Novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer that are capable of prolonging the action of insulin preparations are disclosed.
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- The use of the cyanomethyl unit as a protecting group for phenols, amines and carbamates
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The use of the cyanomethyl unit as a protecting group for phenols, primary and secondary amines, and carbamates is described. Optimized conditions for formation and hydrolysis of cyanomethyl in the presence of the other hydrogenolysis-sensitive groups such as O- and N-benzyl groups are presented.
- Benarab,Boye,Savelon,Guillaumet
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p. 7567 - 7568
(2007/10/02)
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