61396-67-6Relevant articles and documents
Synthesis and aminopeptidase n inhibiting activity of 3-(nitrophenoxymethyl)-[1,3,2]dioxaborolan-2-OLS and their open analogues
Farsa, Oldrich,Kana, Jakub,Macku, Irena,Zelazkova, Jana,Podlipna, Jana,Cirkva, Ales,Maxa, Jaroslav,Stastny, Kamil
, p. 127 - 135 (2017/01/21)
Aminopeptidase N (APN) represents a class of zinc metallopeptidases with broad substrate specifity. This enzyme is involved in control of angioneogenesis in cancer and microvascular conditions. It also serves as a superficial cellular receptor that enables attachment of some viruses including coronaviruses to the host cell. APN takes part also in metabolism of some important neuropeptides. That is why APN can be a promising therapeutic target and compounds which influence its activity interesting potential drugs. Here, synthesis of compounds which in most contain 3-phenoxypropan-1,2 diol moiety and evaluation of their inhibition activity against APN is described. 4-[1-, 2- and 3-(Nitrophenoxymethyl)]-[1,3,2]dioxaborolan-2-ols are novel compounds which have never been previously reported in the literature. 3-(Aminophenoxy)propyl-1,2-diols revealed greater activity than both 3-(nitrophenoxy)propyl-1,2-diols and 3-(nitrophenoxymethyl)-[1,3,2]dioxaborolan-2-ols. A QSAR study revealed a linear correlation between lipophilicity and inhibition activity.
SUBSTITUTED SULFONAMIDE DERIVATIVES
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, (2009/10/22)
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
Substituted Sulfonamide Compounds
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Page/Page column 48, (2009/10/30)
Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.