Two novel fluorine-containing cyclophanes 1 and 2 incorporating a 1,4-bismethylfluorophenylene subunits have been synthesized via the template-directed clipping methodology and their structure was characterized by 1H NMR, 13C NMR, MALDI-TOF-MS and elemental analysis. X-ray diffraction analysis o...
The title molecule (E)-2-[2-(2,6-dichlorophenyl)ethenyl]-8-hydroxyquinoline (DPEQ) was synthesized and characterized by FT-IR, UV–vis, NMR spectroscopy. The molecular geometry, vibrational frequencies and gauge independent atomic orbital (GIAO) 1H and 13C NMR chemical shift values of the compou...
The crystal structure of a new coordination compound tri(2-(2,6-dichlorophenyl)-1H-imidazo[4,5-f][1,10]phenanthroline) Co(II) complex ([Co(dcpip)3]Cl2) was measured with X-ray diffraction measurements. The compound is crystallizes triclinic, Pī space group. The ligand, 2-(2,6-dichlorophenyl)-1H...
Five new 4-substituted arylidene-2-[5-(2,6-dichlorophenyl)-3-methyl-1,2-oxazol-4-yl]-1,3-oxazol-5-ones have been designed and synthesized in order to study their third-order nonlinear optical properties. These novel compounds were characterized by advanced spectroscopic techniques (IR, 1H, 13C N...
5-n-butyl-4-{4-[2-(1H-tetrazole-5-yl)-1H-pyrrol-1-yl]phenylmethyl}-2,4-dihydro-2-(2,6-dichlorophenyl)-3H-1,2,4-triazol-3-one (Ib), a new nonpeptide angiotensin AT1-receptor antagonist, has been observed to play a positive role in the treatment of hypertension in preclinical tests. Four process i...
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enone using structure-based design strategies resulted in inhibitors with considerable improvement in biochemical potency against human lactate dehydrogenase A (LDHA). These potent inhibitors were typically selective for LDHA ...
We have identified potassium 2-nitroimidazole-l-acetohydroxamate (KIH-802) as a hypoxic cell radiosensitizer potentially superior to Miso. The water-soluble acetohydroxamates of 2-nitroimidazole (KIH-802; free acid 801) and 4-nitroimidazole (KIH-852) were designed, synthesized, and evaluated by ...
The anomeric configuration of tyvelose, 3,6-dideoxy-d-arabino-hexopyranose, in the recently discovered glycan epitopes of the parasite Trichinella spiralis has not been established. Two 2-(trimethylsilyl)ethyl disaccharide glycosides, α- and β-Tyv-(1 → 3)-β-d-GalNAc (4 and 5), have been synt...
Perbenzylated methyl α-l-fucopyranosyl-(1→2)-β-d-galactopyranosides having a single free OH group at position C-2′, C-3′ or C-4′ have been synthesized. Methyl 3,4,6-tri-O-benzyl-β-d-galactopyranoside was glycosylated either with phenyl 3,4-di-O-benzyl-2-O-(2-naphthyl)methyl-, phenyl 2,4-d...
The title compound, a protected derivative of a unique component in the moenuronamide group of phosphoglycolipid antibiotics has been synthesised in eleven steps and 30 % total yield from 2(trimethylsilyl) ethyl-β-d-galactopyranoside (6). The key step was a stereroselective addition of methylma...
The glycone part of the flavonoid triglycoside, kaempferol 3-O-β-d-glucopyranosyl-(1→4)-α-l-rhamnopyranosyl-(1→6)-β-d-galactopyranoside, has been synthesized in good yield and stereoselectivity using N-iodosuccinimide and HClO4–silica promoted glycosylations of thioglycoside donors.
A series of N-substituted sulfonylamino-alkanecarboxylate ADAMTS-5 (Aggrecanase-2) inhibitors has been synthesized and the in vitro enzyme SAR is discussed. This report is the first example of carboxylate-based ADAMTS-5 inhibitors which show strong potency of IC50
By using Hf(OTf)4 as the catalyst, a series of 2,3-unsaturated-Se-glucosides have been synthesized for the first time from tri-O-acetyl-d-glucal, 2,4,6-tri-O-benzyl-d-glucal, 3,4-di-O-acetyl-l-rhamnal and ((2R,3S)-3-acetoxy-2,3-dihydrofuran-2-yl) methyl acetate with PhSeH or alkyl(aryl) hydrosel...
Differential thermal analysis (DTA) curves are presented for thorium, scandium, uranium (IV) and the rare-earth metal oxalate hydrates. For all of the metal oxalate hydrates, endothermic and exothermic peaks are present in the curves which are the result of dehydration, decomposition, and oxidat...
Two different air-aged lutetium oxide samples, ex-hydroxide and ex-oxalate, have been characterized by XPS. In the original samples there is an extensive contamination by CO2-3OH- species (O(1s) and C(1s) at 531.6 and 289.4 eV respectively, while the O(1s) peak of O2- ions of the lattice had a B...
One of the world́s most abundant of all the rare earth elements (REE) is cerium. It represents about 50 wt% of total REE content in the main rare earth minerals used industrially (monazite and bastnaesite). However, cerium is not a valuable product if compared with the other REE. In the most cur...
Modulation of the vasoinhibitory effect of NKY-722 by vascular endothelial cells was studied in canine mesenteric arteries. A high concentration of NKY-722 accumulated in the endothelium-intact arteries and its accumulation in endothelium-removed arteries was significantly less. The vasoinhibito...
A new group of 3-(4-substituted-phenyl)-4-(4-methylsulfonamidophenyl)-2(5H)furanones in which the methylsulfonyl (MeSO2) COX-2 pharmacophore present in rofecoxib was replaced by a methanesulfonamido (MeSO2NH) moiety, and where the substituent at the para-position of the C-3 phenyl ring was simul...
Oral cancers are the sixth most frequent cancer with a high mortality rate. Oral squamous cell carcinoma accounts for more than 90% of all oral cancers. Standard methods used to detect oral cancers remain comprehensive clinical examination, expensive biochemical investigations, and invasive biop...
Six denture stomatitis patients, all found to have Candida albicans on their maxillary denture and palatal tissue surfaces, volunteered in this preliminary study to test the in vivo efficacy of human salivary antifungal histidine-rich polypeptides (HRPs) in treating their oral disease. The patie...
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