58754-71-5Relevant academic research and scientific papers
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.
Synthesis and optical storage properties of a thiophene-based holographic recording medium
Matharu, Avtar S.,Jeeva, Shehzad,Huddleston, Patrick R.,Ramanujam
, p. 4477 - 4482 (2008/12/22)
The results of the fabrication and optical data storage characteristics of a novel azothiophene polyester 9 for potential holographic storage are reported. The polyester is derived from an azothiophene diol 1 and diphenyl phthalate 8 via in vacuo melt transesterification. Inclusion of a 5-methoxy-2-thienyl moiety generates a trans π-π* transition centered close to 405 nm. An investigation of the optical data storage characteristics of a solution cast film of azopolyester with a thickness of 65 m is summarised. The optical anisotropy induced by a 532 nm frequency doubled YAG laser and probed at a wavelength of 633 nm outside the absorption band with a polarimeter reveals a very high induced anisotropy of 7 rad (laser intensity, 250 mW cm-2). The calculated birefringence of the film is 0.02 per micron. Maximum anisotropy is reached after approximately 70 s of irradiation. The induced anisotropy disappears at approximately 90 °C. Room temperature stable gratings can be inscribed with high diffraction efficiency. The Royal Society of Chemistry 2007.
Amino naphthyridine compounds as anti-rhoumatic agents
-
, (2008/06/13)
This invention relates to compounds of formula I and pharmaceutically acceptable salts thereof STR1 in which R1 represents hydrogen, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonyalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy alkoxycarbonyl or alkanoylamino; R2 represents hydrogen, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R3 represents hydrogen or alkyl; R4 represents hydrogen, halo, alkoxycarbonyl, a benzyloxycarbonyl, alkanoyl, benzoyl, carbamoyl, alkyl, carboxy, hydroxyalkyl or alkylthio; R5 represents hydrogen or alkyl; R6 represents hydrogen, alkyl [optionally substituted by one or more of the following: hydroxy, halo or an amino group of formula --NR12 R13 ], a C3-12 alicyclic hydrocarbon group, phenyl, (cycloalkyl)alkyl or benzyl; R7 represents hydrogen, halo, trifluoromethyl, trifluoromethoxy, alkyl, carboxy, or alkoxy; R8 represents hydrogen, halo, trifluoromethyl, trifluoromethoxy, alkyl or alkoxy; and R9 represents hydrogen or alkyl; which are antirheumatic agents. Compositions containing these compounds and processes to make them are also disclosed.
