148345-63-5Relevant articles and documents
Bis(carboxyphenyl)-1,2,4-triazole Based Metal-Organic Frameworks: Impact of Metal Ion Substitution on Adsorption Performance
Kobalz,Kobalz,M?llmer,Junghans,Lange,Bergmann,Dietrich,Wecks,Gl?ser,Krautscheid
, p. 6938 - 6948 (2016)
This work presents the syntheses and comprehensive characterization of six paddlewheel based metal-organic frameworks (MOFs) with the general formula ∞ 3[M2L2] (M = Cu, Co, Zn; L = bis(carboxyphenyl)-1,2,4-triazole) forming an isoreticular series with rutile (rtl) topology. These microporous materials are suitable for a systematic investigation of structure-property relationships based on the impact of the metal ion. Depending on the metal ion, the calculated porosities and the pore diameters reach from 58% to 61% and 300 to 750 pm, respectively. Simultaneous thermal analysis and temperature dependent PXRD studies reveal varying thermal behavior with stabilities up to 400 °C. In the case of syntheses with various Co2+/Cu2+, Co2+/Zn2+, and Cu2+/Zn2+ ratios, ICP-OES analyses and SEM-EDX studies confirm the formation of mixed metal MOFs and the metal ion distribution in the bulk samples as well as within the crystals. For the systematic investigation of CO2 (298 K) and N2 (77 K) adsorption properties, all materials were previously subjected to extraction with supercritical CO2. Depending on the metal ion, this procedure causes different phase transitions for each compound. As a result, adsorption studies reveal varying network flexibility for these MOFs. This study is one of the rare examples demonstrating that targeted modification of gate opening pressure, hysteresis shape, and adsorbed amounts of CO2 or N2 are possible by choice of the metal ion. This finding is supported by adsorption studies on the mixed metal MOF ∞3[(Cu0.48Co0.52)2(p-L)2)], showing CO2 adsorption/desorption characteristics of both homonuclear copper and cobalt materials, whereas N2 does not induce gate opening of the framework, as observed for the cobalt MOF. Furthermore, catalytic studies reveal that ∞ 3[Cu2(p-L)2)] is a suitable catalyst for the oxidation of cyclohexene with tert-butylhydroperoxide (TBHP) with high conversion of the starting materials and good selectivity. Its robustness under the applied catalysis conditions leads to similar conversions in repetition measurements.
Design and Synthesis of 3-Carbamoylbenzoic Acid Derivatives as Inhibitors of Human Apurinic/Apyrimidinic Endonuclease 1 (APE1)
Aiello, Francesca,Shabaik, Yumna,Esqueda, Adrian,Sanchez, Tino W.,Grande, Fedora,Garofalo, Antonio,Neamati, Nouri
, p. 1825 - 1839 (2012/10/30)
Apurinic/apyrimidinic (AP) endonuclease 1 (APE1) is a multifaceted protein with an essential role in the base excision repair (BER) pathway. Its implication in tumor development, progression, and resistance has been confirmed in multiple cancers, making it a viable target for intensive investigation. In this work, we designed and synthesized different classes of small-molecule inhibitors of the catalytic endonuclease function of APE1 that contain a 3-carbamoylbenzoic acid scaffold. Further structural modifications were made with the aim of increasing the activity and cytotoxicity of these inhibitors. Several of our compounds were shown to inhibit the catalytic endonuclease function of APE1 with potencies in the low-micromolar range invitro, and therefore represent novel classes of APE1 inhibitors worthy of further development.
CYCLICALLY SUBSTITUTED 3,5-DICYANO-2-THIOPYRIDINES AND USE THEREOF
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Page/Page column 29, (2010/02/17)
The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
Inhibitors of acyl-coA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N- (heteroaryl-substituted benzyl)-N'-arylureas
Tanaka, Akira,Terasawa, Takeshi,Hagihara, Hiroyuki,Sakuma, Yuri,Ishibe, Noriko,Sawada, Masae,Takasugi, Hisashi,Tanaka, Hirokazu
, p. 2390 - 2410 (2007/10/03)
A series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylurea and related derivatives represented by 2 and 3 have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. Among these novel compounds, the type 3 series was superior. A pyrazol-3-yl group on the N-benzyl group of this trisubstituted urea (i.e. 3, Ar1 = pyrazol-3- yl) was identified as a heteroaromatic ring providing a good profile of biological activity. As a result of optimization of the combination with the N-alkyl group (R) and N-aryl group (At3), compound 3aq (FR186054) was identified as a new, orally efficacious ACAT inhibitor, which exhibited potent in vitro ACAT inhibitory activity (rabbit intestinal microsomes IC50 = 99 nM) and excellent hypocholesterolemic effects in cholesterol-fed rats, irrespective of administration mode (ED50 = 0.046 mg/kg dosed via the diet, ED50 = 0.44 mg/kg administered by gavage in PEG400 vehicle). Moreover, a toxicological study revealed compound 3aq to be nontoxic to the adrenal glands of dogs when tested at a single dose of 10 mg/kg po.
Process for the preparation of tetrazoles
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, (2008/06/13)
The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: STR1 or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.
