Search results for "isoxazole"
showing 10 items of 100 documents
On the rearrangement of some Z-arylhydrazones of 3-benzoyl-5-phenylisoxazoles into 2-aryl-4-phenacyl-2H-1,2,3-triazoles: a kinetic study of the subst…
2015
Abstract The rearrangement of eight new Z -arylhydrazones of 3-benzoyl-5-phenylisoxazoles ( 3d – k ) into the relevant 2-aryl-4-phenacyl-2 H -1,2,3-triazoles ( 4d – k ) in dioxane/water solution at different proton concentrations has been quantitatively studied in a wide temperature range (293–333 K). The data collected together with some our previous ones on compounds 3a – c have allowed a deep study of the substituent effects on the course of the rearrangement, thus increasing our knowledge on the Boulton–Katritzky reactions in isoxazole derivatives and on the temperature effects on free energy relationships.
Systemic PaO2 oscillations cause mild brain injury in a pig model
2016
OBJECTIVE: Systemic PaO2 oscillations occur during cyclic recruitment and derecruitment of atelectasis in acute respiratory failure and might harm brain tissue integrity. DESIGN: Controlled animal study. SETTING: University research laboratory. SUBJECTS: Adult anesthetized pigs. INTERVENTIONS: Pigs were randomized to a control group (anesthesia and extracorporeal circulation for 20 hr with constant PaO2, n = 10) or an oscillation group (anesthesia and extracorporeal circulation for 20 hr with artificial PaO2 oscillations [3 cycles min⁻¹], n = 10). Five additional animals served as native group (n = 5). MEASUREMENTS AND MAIN RESULTS: Outcome following exposure to artificial PaO2 oscillations…
Structure-activity relationship studies of novel heteroretinoids: induction of apoptosis in the HL-60 cell line by a novel isoxazole-containing heter…
1999
In a search for retinoic acid receptor (RAR and RXR)-selective ligands, a series of isoxazole retinoids was synthesized and evaluated in vitro in transcriptional activation and competition binding assays for RARs and RXRs. In addition, these compounds were evaluated for their differentiating, cytotoxic, and apoptotic activities. In general, these derivatives showed scarcely any binding affinity and were not active in the transcriptional assay. However, among these isoxazole derivatives, the cis-isomer 14b was identified as a potent inducer of apoptosis, and its activity was found to be 6.5 and 4 times superior than that of 13-cis- and 9-cis-retinoic acids, respectively. On the other hand, c…
The antitumor activities of curcumin and its isoxazole analogue are not affected by multiple gene expression changes in an MDR model of the MCF-7 bre…
2007
We examined the effects of curcumin and of its isoxazole analogue MR 39 in the MCF-7 breast cancer cell line and in its multidrug-resistant (MDR) variant MCF-7R. In comparison with MCF-7, MCF-7R lacks estrogen receptor alpha (ERalpha) and overexpressess P-glycoprotein (P-gp), different IAPs (inhibitory of apoptosis proteins) and COX-2. Through analyses of the effects on cell proliferation, cycling and death, we have observed that the antitumor activity of curcumin and of the more potent (approximately two-fold) MR 39 is at least equal in the MDR cell line compared to the parental MCF-7. Similar results were observed also in an MDR variant of HL-60 leukemia. RT-PCR evaluations performed in M…
Design and synthesis of hybrid drugs based on curcumin scaffold
2012
ChemInform Abstract: Synthesis of 4(5)-Phenacyl-imidazoles from Isoxazole Side-Chain Rearrangements.
2011
The reaction must be carried out under nitrogen atmosphere in deoxygenated solvent to prevent the oxidation of the imidazole products.
CCDC 160804: Experimental Crystal Structure Determination
2001
Related Article: E.Aiello, S.Aiello, F.Mingoia, A.Bacchi, G.Pelizzi, C.Musiu, M.G.Setzu, A.Pani, P.La Colla, M.E.Marongiu|2000|Bioorg.Med.Chem.|8|2719|doi:10.1016/S0968-0896(00)00211-X
CCDC 1917652: Experimental Crystal Structure Determination
2019
Related Article: E.S. Sales, A.J. Bortoluzzi, A.A. Merlo|2019|Acta Crystallogr.,Sect.E:Cryst.Commun.|75|896|doi:10.1107/S2056989019007412
CCDC 148166: Experimental Crystal Structure Determination
2001
Related Article: M.Carda, R.Portoles, J.Murga, S.Uriel, J.A.Marco, L.R.Domingo, R.J.Zaragoza, H.Roper|2000|J.Org.Chem.|65|7000|doi:10.1021/jo0009651
CCDC 148165: Experimental Crystal Structure Determination
2001
Related Article: M.Carda, R.Portoles, J.Murga, S.Uriel, J.A.Marco, L.R.Domingo, R.J.Zaragoza, H.Roper|2000|J.Org.Chem.|65|7000|doi:10.1021/jo0009651