Search results for "Oxazole"

2-Alkenoyl Pyridine N-Oxides, Highly Efficient Dienophiles for the Enantioselective Cu(II)−Bis(oxazoline) Catalyzed Diels−Alder Reaction

2007

2-Alkenoyl pyridine N-oxides are introduced as a new kind of efficient dienophiles for the Cu(II)−bis(oxazoline) (BOX) catalyzed enantioselective Diels−Alder reaction affording higher reactivity and enantioselectivity (ee's up to 96%) than the corresponding nonoxidized 2-alkenoyl pyridines.

Pyrrolocycloheptaoxazole as potent antitumor agents

2016

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…

Prevalence and antibiotic-resistance of Salmonella isolated from beef sampled from the slaughterhouse and from retailers in Dakar (Senegal)

2005

A study was made of Salmonella contamination in beef sampled from a slaughterhouse and from retailers in Dakar, Senegal. The serotypes as well as antibiotic-resistance patterns of the Salmonella isolates were determined. A total of 435 meat samples (236 from the slaughterhouse, 199 from retailers) were tested. Among them, 275 (63%) were positive for Salmonella, 43% (101/236) from the slaughterhouse and 87% (174/199) from the retailers. Furthermore, 97% of the investigated retailers had at least one beef sample contaminated by Salmonella. The 286 Salmonella isolates were divided into 51 serotypes. The most prevalent serotypes were Salmonella bredeney (25%), S. muenster (8%), S. waycross (7%)…

Host-Nonspecific Iron Acquisition Systems and Virulence in the Zoonotic Serovar of Vibrio vulnificus

2014

ABSTRACT The zoonotic serovar of Vibrio vulnificus (known as biotype 2 serovar E) is the etiological agent of human and fish vibriosis. The aim of the present work was to discover the role of the vulnibactin- and hemin-dependent iron acquisition systems in the pathogenicity of this zoonotic serovar under the hypothesis that both are host-nonspecific virulence factors. To this end, we selected three genes for three outer membrane receptors ( vuuA , a receptor for ferric vulnibactin, and hupA and hutR , two hemin receptors), obtained single and multiple mutants as well as complemented strains, and tested them in a series of in vitro and in vivo assays, using eels and mice as animal models. Th…

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 1519195: Experimental Crystal Structure Determination

2017

Related Article: Y. Hernández, I.S. Marcos, N.M. Garrido, F. Sanz, D. Diez|2017|Acta Crystallogr.,Sect.E:Cryst.Commun.|73|85|doi:10.1107/S2056989016019952

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