Search results for "Azole"
showing 10 items of 2392 documents
A frozen analogue approach to aminopyridinylimidazoles leading to novel and promising p38 MAP kinase inhibitors.
2012
In this study we report the design, synthesis, and biological evaluation of constrained aminopyridinylimidazoles as p38α MAP kinase inhibitors. The frozen analogue approach focused on the pyridinyl unit, using purine bioisosteres as constrained structure analogues. The identification of the most potent bioisostere was followed by a further derivatization to address hydrophobic region II. In combination with C-2 modifications of the imidazole core, we were able to design highly active inhibitors on the p38α MAP kinase. The inhibitor design presented herein represents a promising and highly efficient advancement of recent stages of development in this class of p38 MAP kinase inhibitors. In co…
Copper(II) Polyamine Complexes withN-Benzothiazole Sulfonamides as Counterions — Synthesis, Crystal Structures, and Properties of [Cu(dien)2](L1)2[HL…
2003
Copper(II) complexes of new N-benzothiazole sulfonamides (HL1= N-2-(benzothiazole)naphtalensulfonamide and HL2 = N-2-(6-chlorobenzothiazole)toluenesulfonamide) with ethylenediamine (en) and diethylenetriamine (dien) have been synthesized and characterised. The crystal structures of [Cu(dien)2](L1)2 (1) and [Cu(en)2(H2O)2](L2)2 (2) compounds have been determined. The metal centre adopts a “4+2” distorted octahedral environment in both complexes. Unusually, the sulfonamidate anions act as counterions. Spectroscopic properties are in good agreement with the crystal structures. The superoxide dismutase (SOD)-like activity of complex 2 has been tested. Kupfer(II)-Polyamin-Komplexe mit N-Benzothi…
Combination therapy in a model of pulmonary aspergillosis
2009
Summary. The current treatment for pulmonary aspergillosis, amphotericin B, is toxic and not always effective. This study was done to evaluate combinations of amphotericin B with other agents in an animal model of pulmonary aspergillosis. Sprague-Dawley rats were treated with cortisone acetate, infected intratracheally with 106 spores of Aspergillus fumigatus, and followed daily for survival. Mortality among controls started on day 2, and it was 80% by day seven, whereas therapy with amphotericin B resulted in survival of all animals. When given alone, ketoconazole, 5-fluorocytosine and rifampin did not improve survival. The combination of ketoconazole with amphotericin B resulted in comple…
Prophylactic Fluconazole andCandida kruseiInfections
1992
trans-Bis(1H-benzimidazole-1-thione-κS)tetrachlorotellurium methanol disolvate
2002
The Te atom in the title complex, trans-[TeCl4(C6H4N2H2CS)2]·2CH4O or C16H20Cl4N4O2S2Te, occupies a special position at a crystallographic inversion centre and has an octahedral coordination formed by four chloro ligands and the S atoms of two benzimidazole–thione molecules. The hydrogen-bond system involving the disordered solvent methanol molecules links the tellurium complexes into the infinite two-dimensional aggregates in the crystal.
Heterocyclisch anellierte Steroide aus 2-Hydroxymethylen-canrenon
1995
A-ring annulated heterocycles, the isoxazole 6, the pyrazoles 8 and the pyrimidines 9 are prepared starting from 2-hydroxymethylene canrenone 1. Binding studies were carried out with the compounds 1 and 6-8 using estrogen, progesterone, androgen, gluco- and mineralocorticoid receptors as well as the serum proteins SHBG and CBG: the substances were inactive on the receptor level. 1, 7 and 8a show weak binding affinity to CBG.
High resistance against clindamycin, metronidazole and amoxicillin in Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans isolates of …
2010
Objectives: To test the antimicrobial sensitivity of two periodontal pathogens to a panel of five orally administrable antibiotics in periodontal disease. Study design: A total of 69 isolates of Aggregatibacter actinomycetemcomitans and Porphyromonas gingivalis were processed using culture and biochemical tests. Selected colonies of A. actinomycetemcomitans and P. gingivalis were used to evaluate the antibacterial activity of clindamycin, metronidazole, amoxicillin, moxifloxacin and amoxicillin/clavulanic acid. Results: Susceptibility testing revealed a sensitivity of 100% of A. actinomycetemcomitans and P. gingivalis to moxifloxacin and amoxicillin/clavulanic acid but moderate susceptibili…
Study of [2-(2’-pyridyl)imidazole] complexes to confirm two main characteristic thermoanalytical behaviors of transition metal complexes based on imi…
2016
Abstract Imidazole derivative ligands are recognized as useful models for biomimetic complexes. Among the inorganic–organic hybrid complexes, those with derivatives of imidazole heterocyclic N-donor ligands are interesting for their framework. In previous studies of complexes with imidazole derivative ligands, our group reported two main thermally induced decomposition behaviors supporting two different systematic decomposition trends. In this work, one of these characteristic decomposition mechanisms was again found. The final goal of these serial studies is the possibility to provide, by the experimental evidences, a prediction model of thermal stability and decomposition typical behavior…
CCDC 1921767: Experimental Crystal Structure Determination
2019
Related Article: Rezeda Gayfullina, Sirpa Jääskeläinen, Igor O. Koshevoy, Pipsa Hirva|2019|Inorganics|7|87|doi:10.3390/inorganics7070087
CCDC 1434703: Experimental Crystal Structure Determination
2016
Related Article: Christian Köhler and Eva Rentschler|2016|Eur.J.Inorg.Chem.||1955|doi:10.1002/ejic.201501278