We report the solid phase synthesis and some pharmacological properties of seventeen new oxytocin (OT) analogues. Basic modification at positions 8 and/or 9 (introduction of l-α-t-butylglycine [Gly(But)]) was combined with d-Cys6, d-Tyr(Et)2, Mpa1 or Pen1 modifications and their various combina...
Direct administration of either oxytocin or its analogue (1-penicillamine,4-threonine)oxytocin into the preoptic anterior hypothalamus caused hyperthermia in conscious rats at ambient temperatures (Ta's) of 8, 22 and 30°C. At a Ta of 8°C, the hyperthermia was solely brought about by an in...
Three 2,2-dicyanovinyl (DCV) end-capped A-π-D-π-A type oligothiophenes (DCV-OTs) containing dithieno[3,2-b:2′,3′-d]silole (DTSi), cyclopenta[1,2-b:3,4-b′]dithiophene (DTCP) or dithieno[3,2-b:2′,3′-d]pyrrole (DTPy) unit as the central donor part, mono-thiophene as the π-conjugation bridge...
Solid-state emissive organic materials are perspective for applications in organic electronics. Here, the 2,2-dicyanovinyl derivatives bearing thiophene, furan, phenyl, N-methylpyrrole, naphthalene, benzothiophene and benzofuran structures were successfully prepared by the Knoevenagel condensati...
The sensitivity of 73 isolates of Mycosphaerella graminicola collected over the period 1993–2002 from wheat fields in South England was tested in vitro against the triazole fluquinconazole, the strobilurin azoxystrobin and to the imidazole prochloraz. Over the sampling period, sensitivity of th...
Dissipation behaviour of simultaneously applied fungicides fluquinconazole and pyrimethanil was studied in/on apples intended for baby food production (cultivars Jonagold Decosta, Golden and Champion). The apples were sprayed at two dosages to control the pathogen Venturia inaedequalis (Cooke) A...
Mixing fungicides with bacteria that produce antimicrobial compounds is an integrated management tool that can reduce root rot pathogens such as Gaeumannomyces graminis var. tritici (Ggt), which causes take-all disease in wheat. This study analyzed the effect of wheat seed treatments on the surv...
The IR and 1H and 13C NMR spectra of 3-phenethyl-3-azabicyclo[3.2.1]octan-8-α-ol have been studied in several media, and its crystal structure has been determined by X-ray diffraction. The bicyclic system adopts a chair—envelope conformation with both OH and phenethyl groups in equatorial posi...
The enantioselective hydrogenation of (E)-2-(4-methoxy-3-(3-methoxypropoxy)-benzylidene)-3-methylbutanoic acid (1) to (R)-2-(4-methoxy-3-(3-methoxypropoxy)-benzyl)-3-methylbutanoic acid (2)—a key intermediate in the synthesis of the pharmacologically important renin inhibitor Aliskiren—is desc...
Damage of the blood–brain barrier (BBB) during the process of cerebral ischemic injury is a key factor that influences the therapeutic efficacy to the cerebral ischemic injury. This work was designed to investigate the mechanisms underlying the protective effects of 4-methoxy benzyl alcohol (4-...
S-benzyl-β-N-[3-(4-hydroxy-3-methoxy-phenylallylidene)]dithiocarbazate (HL) formed novel complex Bis[S-benzyl-β-N-[3-(4-hydroxy-3-methoxy-phenylallylidene)]dithiocarbazate]zinc(II) having general formula [Zn(HL)2] with (ZnII)-acetate, elucidated by UV-Vis, FT-IR, Raman, 1H-NMR, 13C-NMR, Mass s...
The cytotoxic activity of a new series of 2-(4′-chlorobenzyl)-5,6-disubstituted imidazo[2,1-b][1,3,4]thiadiazoles against different human and murine cancer cell lines is reported. Among the tested compounds, two derivatives namely 2-(4-chlorobenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b][1,3,4...
TEMPO (2,2,6,6-tetramethyl piperidine-1-oxyl) is electrochemically oxidized to a stable form of the cation (TEMPO+) in acetonitrile (CH3CN) or 1-butyl-3-methyl-imidazolium hexafluorophosphate ([BMIm][PF6]) media. Cyclic voltammograms were characterized by a well-defined one-electron reversible r...
A series of 2′-aryl/benzyl-2-aryl-4-methyl-4′,5-bithiazolyl derivatives, 25–64 were synthesized and evaluated for inhibitory activity against Mycobacterium smegmatis MC2 155 strain and antimicrobial activities against four pathogenic bacteria Bacillus subtilis, Staphylococcus aureus, Escheric...
Several novel trans-3-benzyl/(diphenyl)methyl/naphthylseleno substituted monocyclic β-lactams (5–7) have been synthesized in high yields. The reaction scheme inolves [2 + 2] cycloaddition (Staudinger) reaction between suitably substituted imines 4(a–h) and ketenes (B) accessed from 2-benzyl/(...
Benzimidazole derivatives are of substantial importance because of their wide array of pharmacological activities. These nitrogen-containing heterocycles are used as therapeutic agents in medicinal chemistry. The title compound has been prepared using click chemistry (Copper-Catalyzed Azide-Alky...
For the purpose of preparation of optically active aminoalcohol congeners possessing both hydroxyl- and dialkylamino-substituted vicinal chiral carbons, lipase-assisted acylation of methyl (2E,4R*,5S*)-4-(N-benzyl-N-methyl)amino-5-hydroxyhex-2-enoate (4) using CAL-B with vinyl hexanoate as an ac...
N-benzyl-2-methyl-4-nitroaniline (BNA) fiber single crystals were grown by the micro-pulling down (µ-PD) method. Crucible material and its shape were selected based on wetting of the crucible material by liquid BNA. As a result, BNA fiber single crystal with about 1–2 mm diameter was successfu...
Synthesis of the organic nonlinear optical compound N-benzyl-2-methyl-4-nitroaniline (BNA) was carried out in a newer chemical environment using the mixture of benzyl chloride and 2-methl-4-nitroaniline by a preferred laboratory synthesis process. The synthesized BNA compound was separated by co...
Three series of 4-hydroxy-N′-[benzylidene/1-phenylethylidene]-2-H/methyl/benzyl-1,2-benzothiazine-3-carbohydrazide 1,1-dioxides (9–11)a-l were synthesized and unraveled to be highly potent dual inhibitors of monoamine oxidases (MAO-A and MAO-B). All the examined compounds demonstrated IC50 val...
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