Three analogues of the dual μ-/δ-antagonist, H-Dmt-Tic-R-NH-CH2-Ph (R = 1, Lys-Z; 2, Lys-Ac; 3, Lys) were examined in vivo: 1 and 2 exhibited weak bioactivity, while 3 injected intracerebroventricularly was a potent dual antagonist for morphine- and deltorphin C-induced antinociception compara...
Overall rates of polymerization of ring-substituted-N-phenylmaleimides were measured, mainly in dioxane. Rate equations were deduced. The rate of polymerization increased on addition of ZnCl2; the effect was attributed to the interaction of the Lewis acid and the π-cloud of the growing maleimid...
Based on a recent report that 1-methyl-3-phenylpyrrolyl analogues are moderately potent reversible inhibitors of the enzyme monoamine oxidase B (MAO-B), a series of structurally related N-methyl-2-phenylmaleimidyl analogues has been prepared and evaluated as inhibitors of MAO-B. In general, the ...
Antiproliferative activity of twenty-nine (E)-4-aryl-4-oxo-2-butenoic acid amides against three human tumor cell lines (HeLa, FemX, and K562) is reported. Compounds showed antiproliferative activity in one-digit micromolar to submicromolar concentrations. The most active derivatives toward all t...
The hydrolytic stability of norcantharidine derived conformationally constrained diamides in acidic media is solely governed by the type of amide. Tertiary diamides underwent smooth acid catalyzed hydrolysis due to anchimeric assistance whereas other diamides were stable. This was corroborated f...
Different esters of 3-(4′-geranyloxy-3′-methoxyphenyl)-2-trans propenoic acid (1), an anti-inflammatory principle of Acronychia baueri Schott (Rutaceae), were synthesized. Their topical anti-inflammatory activity was evaluated using the Croton oil ear test in mice as a model of acute inflammat...
Several series of methyl- and fluoro-substituted polycyclic aromatic hydrocarbon (PAH) derivatives were tested for mutagenic activity in cell-mediated assays with cells of the human hepatoma cell line, HepG2, as PAH activators. The mutagenic activity of dibenz[a, h]anthracene [DB(a,h)A] increase...
Female NIH Swiss mice were treated topically with either 0.01 or 0.1 μmol 7,12-[3H]dimethylbenz[a]anthracene and DNA was isolated either from the whole skin, the dermis or the epidermis. Levels of binding to DNA and levels of individual adducts formed were similar in all 3 tissue fractions for ...
Polar, ethyl acetate soluble metabolites formed in incubations of dibenz[a,c]-anthracene (DB[a,c]A), dibenz[a,h]anthracene (DB[a,h]A) and the related DB[a,h]A 3,4-diol and dibenz[a,j]anthracene (DB[a,j]A) with 3-methylcholanthrene (3-MC)-induced rat liver microsomal preparations have been separa...
We report new examples of a series of losartan–hydrocaffeic hybrids that bear novel ester, amide and amine linkers. These compounds were made by linking hydrocaffeic acid to the side chain of losartan at the C-5 position of the imidazole ring through different strategies. Experiments performed ...
Concentrations of 13 organophosphate ester flame retardants (OPEs) were measured in air, dust and window wipes from 63 homes in Canada, the Czech Republic and the United States in the spring and summer of 2013 to look for abundances, differences among regions, and partitioning behavior. In gener...
Organophosphate esters (OPEs) are used as flame retardants and plasticizers in a wide range of consumer products. Nevertheless, studies on the occurrence and inventory of OPEs in sewage sludge are limited. In this study, 20 OP triesters and 11 diesters were measured in 75 archived sewage sludge ...
Biocatalysis exhibits distinct improvement as compared to the chemical method of synthesis with respect to simplification of operating process, improvement in end product quality and minimization of by-product. However, long duration of synthesis, slow reaction rate and poor conversion limit the...
The intraperitoneal injection of methylglyoxal bis(cyclohexylamidinohydrazone) (MGBC), an inhibitor of S-adenosylmethionine decarboxylase and spermidine synthase, markedly increased (7-fold of the basal level at 4 hr) ornithine decarboxylase (ODC) activity in normal mouse liver. ODC activity was...
A complete series of analogs of tyrosine modified neurokinin A ([Tyr1]-NKA or [Tyr0]-NKA) has been synthesized by substituting each natural residue with l-Cys. These analogs were tested for their ability to bind recombinant neurokinin-2 (NK-2) receptor. Substitution of Phe6 with Cys completely a...
Discovered in 1983, the decapeptide neurokinin A has been shown to occur in several peripheral organs and to exert a variety of biological effects. In this article, we review the most sensitive and selective in vivo and in vitro tests which have been used in various laboratories to evaluate natu...
Analogues highly selective for receptors for substance P [β-Ala4,Sar9,Met(02)11]-SP(4–11), for neurokinin A, [Nle10]-NKA(4–10), and for neurokinin B, [β-Asp4,MePhe7]-NKB(4–10), were administered intraarterially before and after atropine or tetrodotoxin, to characterize the locations on nerv...
The classical tachykinins, substance P, neurokinin A and neurokinin B are predominantly found in the nervous system where they act as neurotransmitters and neuromodulators. Significantly reduced levels of these peptides were observed in neurodegenerative diseases and it may be suggested that thi...
A structure-activity study of the neurokinin A (NKA) fragment NKA(4–10) was performed to investigate the importance of amino acid residues for receptor efficacy, potency and affinity at the NK2 receptor in human colon circular muscle. Fourteen analogs of NKA(4–10) were produced with substituti...
While a batch of efforts are fastened on synthesizing the novel targeted anti-cancer agents, recent investigations have achieved a breakthrough in identifying a favorable anti-tumor activity for some supportive drugs, which their safety have been confirmed thus far. The results of the present st...
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