ENZYME INHIBITION BY DERIVATIVES OF PHENOTHIAZINE VI. INHIBITION OF GLYOXALASE ACTIVITY OF HUMAN AND RABBIT ERYTHROCYTES

1953 ◽  
Vol 31 (3) ◽  
pp. 195-201
Author(s):  
H. B. Collier ◽  
Sheila C. McRae
Keyword(s):  
Methylene Blue ◽  
Enzyme Inhibition ◽  
Strong Inhibitor ◽  
Intact Cells ◽  
Relationship Of ◽  
Derivatives Of

Phenothiazone has been found to be a strong inhibitor of glyoxalase activity of human and rabbit erythrocytes. Concentrations for 50% inhibition were 10−6 M for intact cells and 10−4 M for haemolysates with added glutathione. Glyoxalase activity was also markedly inhibited by phenothiazine, methylene blue, and p-chloromercuribenzoate; slightly inhibited by alloxan and phenylhydrazine; and not affected by dialuric acid. Enzyme inhibition did not parallel methaemoglobin formation. The possible relationship of these findings to the haemolytic action of phenothiazine is discussed.

ENZYME INHIBITION BY DERIVATIVES OF PHENOTHIAZINE: II. INHIBITION OF CHOLINESTERASE

1942 ◽  
Vol 20b (9) ◽  
pp. 189-193 ◽  
Author(s):  
H. Bruce Collier ◽  
Della E. Allen
Keyword(s):  
Methylene Blue ◽  
Alkaline Phosphatase ◽  
Enzyme Inhibition ◽  
Cholinesterase Activity ◽  
Horse Serum ◽  
Phenothiazine Derivatives ◽  
Serum Lipase ◽  
Derivatives Of

The cholinesterase activity of horse serum is strongly inhibited by phenothiazone and by some phenothiazine alkyl-sulphonium salts. The magnitude of this inhibition is about equal to that produced by methylene blue and by acriflavine. Alkaline phosphatase and serum lipase are not affected.The possible relation of this property of phenothiazine derivatives to certain nervous symptoms observed in treated pigs, and to insecticidal and anthelmintic action, is discussed.

ENZYME INHIBITION BY DERIVATIVES OF PHENOTHIAZINE: VII. INHIBITION OF GLUCOSE-6-PHOSPHATE DEHYDROGENASE ACTIVITY OF RABBIT ERYTHROCYTES

1965 ◽  
Vol 43 (1) ◽  
pp. 105-110 ◽  
Author(s):  
H. B. Collier ◽  
M. W. Gray
Keyword(s):  
Methylene Blue ◽  
Dehydrogenase Activity ◽  
Enzyme Inhibition ◽  
Enzyme System ◽  
Spectrophotometric Assay ◽  
Direct Oxidation ◽  
Phenothiazine Derivatives ◽  
Dye Reduction ◽  
Glucose 6 Phosphate Dehydrogenase ◽  
Derivatives Of

The effects of various phenothiazine derivatives were tested, by a NADP+-coupled spectrophotometric assay, on the glucose-6-phosphate dehydrogenase activity of hemolysates of rabbit erythrocytes. Phenothiazine, phenothiazine sulfoxide, thionol, promazine, chlorpromazine, and methylene blue were relatively weak inhibitors. Powerful inhibitors (concentration, for 50% inhibition, I50, in parentheses) were phenothiazone (90 μM) and New Methylene Blue N (75 μM). These two compounds caused a slow direct oxidation of NADPH; however, they appeared to exert an action on the enzyme as well. The enzyme was not inhibited by 2,6-dichlorophenol–indophenol, which is employed in a dye-reduction assay.The enzyme system was readily inactivated by ethanol (I5o = 1.4 M). Prior addition of NADP+ afforded some protection.

ENZYME INHIBITION BY DERIVATIVES OF PHENOTHIAZINE

1952 ◽  
Vol 30 (6) ◽  
pp. 549-551
Author(s):  
G. M. Allenby ◽  
H. B. Collier
Keyword(s):  
Rat Brain ◽  
Brain Tissue ◽  
Enzyme Inhibition ◽  
Anthelmintic Activity ◽  
Hexokinase Activity ◽  
Relationship Of ◽  
Derivatives Of ◽  
Rat Brain Tissue

Rat-brain tissue was homogenized in the presence of fluoride to depress apyrase, and hexokinase activity of the homogenate was measured manometrically. Phenothiazone was found to be a powerful inhibitor of hexokinase, with 50% inhibition at about 7 × 10−6 M concentration. The possible relationship of this finding to the anthelmintic activity of phenothiazine is discussed.

On derivatives of fuzzy multi-dimensional mappings and applications under generalized differentiability

2021 ◽  
pp. 1-19
Author(s):  
M. Miri Karbasaki ◽  
M. R. Balooch Shahriari ◽  
O. Sedaghatfar
Keyword(s):  
Linear Function ◽  
Level Set ◽  
Fuzzy Numbers ◽  
Sufficient Condition ◽  
Continuous Linear ◽  
Generalized Differentiability ◽  
Relationship Of ◽  
The Relationship ◽  
Derivatives Of ◽  
Dimensional Mapping

This article identifies and presents the generalized difference (g-difference) of fuzzy numbers, Fréchet and Gâteaux generalized differentiability (g-differentiability) for fuzzy multi-dimensional mapping which consists of a new concept, fuzzy g-(continuous linear) function; Moreover, the relationship between Fréchet and Gâteaux g-differentiability is studied and shown. The concepts of directional and partial g-differentiability are further framed and the relationship of which will the aforementioned concepts are also explored. Furthermore, characterization is pointed out for Fréchet and Gâteaux g-differentiability; based on level-set and through differentiability of endpoints real-valued functions a characterization is also offered and explored for directional and partial g-differentiability. The sufficient condition for Fréchet and Gâteaux g-differentiability, directional and partial g-differentiability based on level-set and through employing level-wise gH-differentiability (LgH-differentiability) is expressed. Finally, to illustrate the ability and reliability of the aforementioned concepts we have solved some application examples.

New 4-Hydroxypyridine and 4-Hydroxyquinoline Derivatives as Inhibitors of NADH-ubiquinone Reductase in the Respiratory Chain

1989 ◽  
Vol 44 (7-8) ◽  
pp. 609-616 ◽  
Author(s):  
Kun Hoe Chung ◽  
Kwang Yun Cho ◽  
Yasuko Asami ◽  
Nobutaka Takahashi ◽  
Shigeo Yoshida
Keyword(s):  
Electron Transport ◽  
Respiratory Chain ◽  
Side Chain ◽  
Pyridine Derivatives ◽  
Transport Function ◽  
Optimal Length ◽  
Structure Activity ◽  
Membrane Effect ◽  
Relationship Of ◽  
Derivatives Of

Many derivatives of 2,3-dim ethoxy-4-hydroxypyridine, which were designed from examination of the structure-activity relationship of piericidins, were tested for inhibition of NADH-UQ reductase. The lipophilic side chain of those compounds was indicated to be a key part for activity and its optimal length was conjectured. By the use of two different phases of assay material, intact mitochondria and submitochondria, the size of a membrane effect was shown to depend on the structure of the side chain. 4-Hydroxyquinoline derivatives were also tested for an analogous role in relation to the electron transport function of menaquinone, and they were proven to be inhibitors of NADH-UQ reductase as good as the pyridine derivatives.

scholarly journals Synthesis and Olfactory Characteristics of Hydroxyether Derivatives of Methyl Eugenol

2020 ◽  
Vol 24 (9) ◽  
pp. 1503-1507
Author(s):  
S.O. Okopi ◽  
L.M. Affiku
Keyword(s):  
Double Bond ◽  
Essential Oils ◽  
Plant Species ◽  
Chemical Transformation ◽  
Structural Modification ◽  
Methyl Eugenol ◽  
Naturally Occurring ◽  
Relationship Of ◽  
Derivatives Of ◽  
Functional Alteration

Methyl eugenol is a naturally occurring substance found in the essential oils of several plant species. It is a cheap and abundant material with a rather limited interest as perfuming ingredient. This research investigated the structure-odour relationship of methyl eugenol and its derivatives, focusing on the chemical transformation of the double bond to hydroxyether derivatives in a controlled manner. Two derivatives 2-(4-ethyl- 3-methoxybenzyl)oxirane (68.8% yield) and 1-(3,4-dimethoxyphenyl)-3-ethoxypropan-2-ol (63.58% yield), were synthesized from methyl eugenol. This research found that the odour characteristic of 2-(4-ethyl-3-methoxybenzyl)oxirane[floral, fresh, slight lime and sweet]compounds, is clearly different from the odours of the 1-(3,4-dimethoxyphenyl)-3-ethoxypropan-2-ol [Glue-like, pungent, and Caramel-like]. It is evident from our observations that double bond substitution and functional alteration of the methyl eugenol modifies the perceived odour of methyl eugenol  derivative. Thus, structural modification overall led to an increase in odour potency. Keywords: Fragrance, Methly-Eugenol, Ether, Olfactory characteristic, Epoxidation.

scholarly journals Synthesis, Spectral and Enzyme Inhibition Studies on N-Aralkyl/ Aryl Sulfonated Derivatives of Commercially Available Paroxetine

2014 ◽  
Vol 26 (1) ◽  
pp. 93-98
Author(s):  
Asia Siddiqa ◽  
Aziz-ur-Rehman ◽  
Muhammad Athar Abbasi ◽  
Shahid Rasool ◽  
Ghulam Hussain ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Inhibition Studies ◽  
Derivatives Of

INCORPORATION OF INORGANIC P32INTO PHOSPHOLIPIDS OF BRAIN SLICES: EFFECT OF CERTAIN TRANQUILLIZING DRUGS

1963 ◽  
Vol 41 (1) ◽  
pp. 1155-1162 ◽  
Author(s):  
W. L. Magee ◽  
R. J. Rossiter
Keyword(s):  
Methylene Blue ◽  
Guinea Pig ◽  
Aerobic Glycolysis ◽  
Brain Slices ◽  
Inorganic P ◽  
Pig Brain ◽  
Low Concentrations ◽  
High Concentrations ◽  
Derivatives Of ◽  
Guinea Pig Brain

Promazine, promethazine, tetrameprazine, and WY 1172, four tranquillizing drugs that are derivatives of phenothiazine, resembled chlorpromazine in that when they were added in a concentration of 0.1 mM to slices of guinea pig brain respiring in a suitable medium they stimulated the incorporation of inorganic P32into the phospholipids of the slices. With one of the drugs, promethazine, this concentration of 0.1 mM was found to cause no significant increase in respiration, in aerobic glycolysis, or in the concentration of phosphocreatine. In higher concentrations (1.0 mM), all of the compounds inhibited the labelling of phospholipid. Promethazine caused a reduction in respiration and in the concentration of phosphocreatine, accompanied by an increase in aerobic glycolysis. Methylene blue, a derivative of phenothiazine with no reported tranquillizing properties, did not stimulate the labelling of phospholipid in brain slices. Azacyclonol, pipradrol, and mepazine, drugs that are derivatives of piperidine, also stimulated phospholipid labelling in low concentrations and inhibited the labelling at higher concentrations. Piperidine and benzhydrol, the two components from which azacyclonol is derived, did not stimulate phospholipid labelling at the concentration which was most effective for azacyclonol. Low concentrations of benzhydrol, however, caused a slight stimulation. Meprobamate and phenaglycodol, two other compounds with reputed tranquillizing action, had either little or no effect. Most of the substances tested inhibited phospholipid labelling when they were added in sufficiently high concentrations.

scholarly journals Development of Perylene-Based Non-Fullerene Acceptors through Bay-Functionalization Strategy

Materials ◽  
2020 ◽  
Vol 13 (9) ◽  
pp. 2148 ◽  
Author(s):  
Keisuke Fujimoto ◽  
Masaki Takahashi ◽  
Seiichiro Izawa ◽  
Masahiro Hiramoto
Keyword(s):  
Material Research ◽  
High Electron ◽  
High Electron Affinity ◽  
History Of ◽  
Synthetic Methodologies ◽  
Molecular Semiconductors ◽  
Relationship Of ◽  
Derivatives Of ◽  
Molecular Nanostructures ◽  
Tremendous Impact

Perylene has had a tremendous impact in the history of material research for the molecular semiconductors. Among numerous derivatives of this polyaromatic hydrocarbon, perylene diimide (PDI) represents a promising class of organic materials envisioned as non-fullerene acceptors (NFAs) for the practical organic photovoltaic (OPV) applications due to their enhanced photo- and thermal stability and remarkably high electron affinity, some of which realize band-like transport properties. The present review guides some of the representative achievements in the development of rationally designed PDI systems, highlighting synthetic methodologies based on bay-functionalization strategies for creating well-designed molecular nanostructures and structure-performance relationship of perylene-based small molecular acceptors (SMAs) for the photovoltaic outcomes.

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