- Metal-Free Synthesis of N-Aryl Amides using Organocatalytic Ring-Opening Aminolysis of Lactones
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Catalytic ring-opening of bio-sourced non-strained lactones with aromatic amines can offer a straightforward, 100 % atom-economical, and sustainable pathway towards relevant N-aryl amide scaffolds. Herein, the first general, metal-free, and highly efficient N-aryl amide formation is reported from poorly reactive aromatic amines and non-strained lactones under mild operating conditions using an organic bicyclic guanidine catalyst. This protocol has high application potential as exemplified by the formal syntheses of drug-relevant molecules.
- Guo, Wusheng,Gómez, José Enrique,Martínez-Rodríguez, Luis,Bandeira, Nuno A. G.,Bo, Carles,Kleij, Arjan W.
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p. 1969 - 1975
(2017/05/16)
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- Antineoplastic application of nitrogen oxides as novel histone deacetylase inhibitor
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The invention discloses antineoplastic application of nitrogen oxides as a novel histone deacetylase inhibitor. The nitrogen oxides have a general structural formula as shown in a formula (I) and show potential inhibitory effect on HDAC. Thus, more nitrogen and oxygen can be provided for a ZBG part, observation can be carried out on a plurality of lengths of linker, and structural modification can be implemented on the basis of prior art so as to find out inhibitors with good selectivity on HDAC subtypes and action of the inhibitors on other targets. The nitrogen oxides provided by the invention has the advantages of cheap synthesis raw materials, simple process, high purity, low cost, etc. and are expected to be developed into novel HDAC inhibitor-series antitumor drugs with good selectivity on HDAC subtypes, high efficiency and low toxicity.
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Paragraph 0040; 0041; 0043; 0045
(2017/10/13)
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- Targeting mycobacterium protein tyrosine phosphatase B for antituberculosis agents
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Protein tyrosine phosphatases are often exploited and subverted by pathogenic bacteria to cause human diseases. The tyrosine phosphatase mPTPB from Mycobacterium tuberculosis is an essential virulence factor that is secreted by the bacterium into the cytoplasm of macrophages, where it mediates mycobacterial survival in the host. Consequently, there is considerable interest in understanding the mechanism by which mPTPB evades the host immune responses, and in developing potent and selective mPTPB inhibitors as unique antituberculosis (antiTB) agents. We uncovered that mPTPB subverts the innate immune responses by blocking the ERK1/2 and p38 mediated IL-6 production and promoting host cell survival by activating the Akt pathway. We identified a potent and selective mPTPB inhibitor I-A09 with highly efficacious cellular activity, from a combinatorial library of bidentate benzofuran salicylic acid derivatives assembled by click chemistry. We demonstrated that inhibition of mPTPB with I-A09 in macrophages reverses the altered host immune responses induced by the bacterial phosphatase and prevents TB growth in host cells. The results provide the necessary proof-of-principle data to support the notion that specific inhibitors of the mPTPB may serve as effective antiTB therapeutics.
- Zhou, Bo,He, Yantao,Zhang, Xian,Xu, Jie,Luo, Yong,Wang, Yuehong,Franzblau, Scott G.,Yang, Zhenyun,Chan, Rebecca J.,Liu, Yan,Zheng, Jianyu,Zhang, Zhong-Yin
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scheme or table
p. 4573 - 4578
(2010/10/03)
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- 1-[(N-(un)substituted)amidoalkyl]spiroindolinonaphthoxazines, their preparation, compositions and (co)polymer matrices containing them
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The object of the present invention is novel spiroindolinonaphthoxazine compounds as well as the compositions and (co)polymer matrices containing them. Said compounds have interesting photochromic properties. Another object of the present invention is a method of preparing said novel compounds.
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- Facile preparation of 2-imino tetrahydrofurans, pyrans and oxepans
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A simple and convenient route to 2-imino tetrahydrofurans, pyrans and oxepans which utilizes a silver-assisted intramolecular O-alkylation has been developed and produces these novel imidates in good yields and with high stereoselectivity.
- Alanine,Fishwick,Szantay Jr.
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p. 6571 - 6572
(2007/10/02)
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