Search results for "ZOL"
showing 10 items of 4792 documents
ChemInform Abstract: Researches on Antiinflammatory Agents. Studies on Some New 3-(Pyrazol-5-yl)-1,2,3-benzotriazin-4(3H)-ones and -quinazolin-4(3H)-…
2010
Following our research on analgesic and antiinflammatory active compounds containing the pyrazole nucleus, a number of 3-(pyrazol-5-yl)-1,2,3-benzotriazin-4(3H)-ones and quinazolin-4(3H)-ones was synthetized and tested. The results of tests for analgesic, antiexudative and antioedema activities, as well as for induction of lesion in the gastric mucosa, are reported and discussed.
Novel insights on [1,2]oxazolo[5,4‐e]isoindoles on multidrug resistant acute myeloid leukemia cell line
2022
A series of [1,2]oxazolo[5,4‐e]isoindole derivatives was evaluated against HL‐60 cell line and its multidrug resistance (MDR) variant, HL‐60R, resistant to doxorubicin and to other P‐gp substrates by overexpressing the efflux pump. They displayed antiproliferative activities, with IC50 values ranging from 0.02 to 5.5μM. In particular, the newly synthesized compound 4k produced synergistic effects in terms of cell growth inhibition and cell death induction either in combination with a Vinca alkaloid, Vinblastine, and a Taxane, Paclitaxel in HL‐60R cells. The study of the mechanism of action indicated that all compounds showed antimitotic activity through inhibition of tubulin polymerization.…
Effect of imidazo[1,2-α]pyrimidine derivatives on leukocyte function
2001
Objective and Design: A series of six imidazo[1,2-α]pyrimidine (IP) derivatives were evaluated for their effects on leukocyte functions in vitro as well as on the inflammatory response induced by zymosan in the mouse air pouch.¶Materials and Subjects: Human neutrophils and murine peritoneal macrophages were used for in vitro assays. Mouse air pouch was performed in Swiss mice.¶Treatment: Test compounds were incubated with either human neutrophils or mouse peritoneal macrophages at concentrations not showing cytotoxic effects. For in vivo experiments, IPs were injected into the air pouch.¶Methods: Elastase and myeloperoxidase release, superoxide generation and LTB4 production were assayed in…
Effects of some isoxazolpyrimidine derivatives on nitric oxide and eicosanoid biosynthesis
2000
Abstract The inhibitory effect of some isoxazolpyrimidine derivatives on iNOS and COX-2 endotoxin induction in mouse peritoneal macrophages has been studied. Three of these compounds inhibited nitrite and PGE2 accumulation in a concentration dependent-manner at μM range. None of these active compounds affected iNOS, COX-2, COX-1 or PLA2 activities, although some reduced iNOS or COX-2 expression. Besides, no effect was observed on human neutrophil inflammatory responses (LTB4 biosynthesis and Superoxide or elastase release). Active compounds were assayed by oral administration in the mouse air pouch model, where they inhibited nitrite accumulation without affecting PGE 2 levels or leukocyte …
Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: The nitroindazolinone chemotype
2011
In this report, we propose the combination of computational methods and in vivo primary screening in zebrafish larvae and confirmatory in mice models as a novel strategy to accelerate anti-inflammatory drug discovery. Initially, a database of 1213 organic chemicals with great structural variability - 587 of them anti-inflammatory agents plus 626 compounds with other clinical uses - was divided into training and test groups. Atom-based quadratic indices - a TOMOCOMD-CARDD molecular descriptors family - and linear discriminant analysis (LDA) were used to develop a total of 13 models to describe the anti-inflammatory activity. The best model (Eq. (13)) shows an accuracy of 87.70% in the traini…
HSP27 controls GATA-1 protein level during erythroid cell differentiation.
2010
AbstractHeat shock protein 27 (HSP27) is a chaperone whose cellular expression increases in response to various stresses and protects the cell either by inhibiting apoptotic cell death or by promoting the ubiquitination and proteasomal degradation of specific proteins. Here, we show that globin transcription factor 1 (GATA-1) is a client protein of HSP27. In 2 models of erythroid differentiation; that is, in the human erythroleukemia cell line, K562 induced to differentiate into erythroid cells on hemin exposure and CD34+ human cells ex vivo driven to erythroid differentiation in liquid culture, depletion of HSP27 provokes an accumulation of GATA-1 and impairs terminal maturation. More spec…
Spin crossover in hexakis(1-(2-chloroethyl)-tetrazole)iron(II) complexes; synthesis and magnetic properties
2002
Abstract The spin-crossover complexes [Fe(teec)6](X)2 (with teec=1-(2-chloroethyl)-tetrazole and X=BF4, ClO4, PF6) possess two iron(II) sites each having a different spin-crossover behaviour. The magnetic behaviour of the complexes obtained by slow crystallisation differs strongly from those obtained by precipitation. This difference results in either a spin crossover of 50% (X=ClO4, crystalline), two gradual steps (X=BF4, PF6), or two steps, of which one is gradual and the other having a thermal hysteresis (X=ClO4 precipitated). Both 57Fe Mossbauer spectroscopy and magnetic susceptibility measurements have been recorded as a function of T. The crystal structure of [Fe(teec)6](BF4)2 has bee…
Synthesis and chemical characterization of CuII, NiII and ZnII complexes of 3,5-bis(2′-pyridyl)-1,2,4-oxadiazole and 3-(2′-pyridyl)5-(phenyl)-1,2,4-o…
2011
Abstract The synthesis and structural characterization of Ni II , Cu II and Zn II complexes of two chelating 1,2,4-oxadiazole ligands, namely 3,5-bis(2′-pyridyl)-1,2,4-oxadiazole (bipyOXA) and 3-(2′-pyridyl)5-(phenyl)-1,2,4-oxadiazole (pyOXA), is here reported. The formed hexacoordinated metal complexes are [M(bipyOXA) 2 (H 2 O) 2 ](ClO 4 ) 2 and [M(pyOXA) 2 (ClO 4 ) 2 ], respectively (M = Ni, Cu, Zn). X-ray crystallography, 1 H and 13 C NMR spectroscopy and C, N, H elemental analysis data concord in attributing them an octahedral coordination geometry. The two coordinated pyOXA ligands assume a trans coplanar disposition, while the two bipyOXA ligands are not. The latter result is a possib…
Coordination behaviour of methazolamide [N(-4-methyl-2-sulfamoyl-Δ2-1,3,4-thiadiazolin-5-ylidene)] acetamide, an inhibitor of carbonic anhydrase enzy…
1993
Abstract The interaction of methazolamide (Hmacm) with Ni(II) ion and ammonia molecules gives rise to the complex of formula [Ni(macm)2(NH3)4]. The complex crystallizes in the monoclinic P21/n space group with a = 14.255(4), b = 7.126(2), c = 12.444(3) A, β = 113.12(3)° and Z = 2. The structure was refined to R = 0.065 (Rw = 0.065). The complex consists of monomeric units which interact through hydrogen bonds and van der Waals contacts. The Ni(II) ion is coordinated with the deprotonated sulfonamido nitrogen of the macm− ligand in axial sites and the ammonia molecules in equatorial positions. IR, electronic spectra and 1H NMR results are also reported.
Mononuclear and binuclear copper(II) complexes with bis(2-imidazolyl)(bis(methoxycarbonyl)methylmethane) (BIBM), a tripodal bis(imidazole) based liga…
2013
Two new Cu(II) complexes with bis(2-imidazolyl) (bis(methoxycarbonyl)methylmethane) (BIBM), a tridentate bis(imidazole) based ligand with the formula [Cu(BIBM) 2 ](ClO 4 ) 2 ( 1 ) and [{Cu(BIBM)(H 2 O)} 2 (μ 1,2,3,4 -C 2 O 4 )](C 4 O 4 )·6H 2 O ( 2 ) have been synthesized and characterized. Compound 1 shows mononuclear cationic [Cu(BIBM) 2 ] 2+ units and perchlorate ions. The coordination around the Cu(II) ion shows a tetragonally-elongated octahedral geometry. The BIBM ligand acts as a k 3 -N,N’,O tripodal ligand, through two imidazole N atoms and a weak Cu–O(carboxymethyl) axial interaction. In the crystal structure cations and anions connect through H-bonds generating linear chains. Line…