88089-95-6Relevant academic research and scientific papers
Double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as preparation method and application thereof, pharmaceutical composition and medicament
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Paragraph 0494-0496, (2021/06/09)
The invention discloses a double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as a preparation method and application thereof, a pharmaceutical composition and a medicament, and belongs to the
Rapid assembly and in situ screening of bidentate inhibitors of protein tyrosine phosphatases
Srinivasan, Rajavel,Uttamchandani, Mahesh,Yao, Shao Q.
, p. 713 - 716 (2007/10/03)
We have successfully designed and synthesized a small library of protein tyrosine phosphatase (PTP) inhibitors, in which the so-called "click chemistry" or Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction was carried out for rapid assembly of 66 different bidentate compounds. Subsequent in situ enzymatic screening revealed a potential PTP1B inhibitor (IC50 = 4.7 μM) which is 10-100 fold more potent than other PTPs.
Substituted N-arylazetidinones, β-lactamases potential inhibitors
Zrihen,Labia,Wakselman
, p. 307 - 314 (2007/10/02)
Two classes of substituted N-aryl azetidinones have been prepared by cyclization of various β-bromopropionanilides. The 7a class possess a carboxylic function in ortho, meta or para of the nitrogen and possibly another alkyl substituent on the aromatic nucleus. In the 7a class, the aromatic nucleus is substituted by a bromomethyl group instead of the alkyl one. Few of these azetidinones show a good affinity for various cell-free β-lactamases preparations, and thus are pretty good competitive inhibitors. Nevertheless, they do not act synergistically with ampicillin on β-lactamase producing bacterial strains. A poor antibacterial activity has been detected for few compounds. The azetidinones 7b which possess a latent electrophilic quinonimine methide function, do not give any progressive (suicide type) inhibition, or inactivation, of the enzymatic activity.
