Aminoalkylidene and aminoalkyl derivatives of 6,11-dihydrodibenzo[b,e]thiepin-2- and -9-carbonitrile and 4,10-dihydrothieno[2,3-c]-1-benzothiepin-6-carbonitrile; Antidepressants with a new activity profile

1988 ◽  
Vol 53 (2) ◽  
pp. 340-360 ◽  
Author(s):  
Karel Šindelář ◽  
Jiří Holubek ◽  
Oluše Matoušová ◽  
Emil Svátek ◽  
Martin Valchář ◽  
...  
Keyword(s):  
Ethyl Chloroformate ◽  
Biochemical Tests ◽  
Hexamethylphosphoric Triamide ◽  
Geometrical Isomers ◽  
Saturated Compound ◽  
Cuprous Cyanide ◽  
The Individual ◽  
Mild Hydrolysis ◽  
Derivatives Of ◽  
Cyano Compounds

Starting from the bromo ketones VIIc, XIII, and XXIV and proceeding via the alcohols VIIIc, IXc, XIV, XVII, and XXVI, the olefinic compounds IIc (+ VI), Xc (+XI), XVc and XIXc(+XXc), and the saturated compound XVIc were prepared. The pairs of geometrical isomers were separated by crystallization of salts and the individual compounds Iic, Xc, XVc, XVIc, XIXc, and XXc were transformed by treatment with cuprous cyanide in hexamethylphosphoric triamide to the corresponding cyano compounds IIb, Xb, XVb, XVIb, XIXb, and XXb. Compound IIb was synthesized also from the ketone VIIc via the cyano ketone VIIb and the cyano carbinol VIIIb. The secondary amine IIIb was prepared from IIc by partial demethylation with ethyl chloroformate, the following hydrolysis to IIIc, protection of NH group with butyrolactone, the following treatment with cuprous cyanide, and deprotection by mild hydrolysis. The title compounds, which are the cyano analogues of antidepressants of the prothiadene series, showed in pharmacological and biochemical tests properties of potential antidepressants and more or less selective inhibitors of the 5-hydroxytryptamine uptake in the rat brain; at the same time they are rather strong central cholinolytics.

The role of secondary alcoholic groups of D-galacturonan in its degradation with exo-D-galacturonanase

1980 ◽  
Vol 45 (2) ◽  
pp. 427-434 ◽  
Author(s):  
Kveta Heinrichová ◽  
Rudolf Kohn
Keyword(s):  
Acetyl Derivative ◽  
Competitive Inhibitor ◽  
Hydroxyl Groups ◽  
Pectic Acid ◽  
Substrate Complex ◽  
Enzyme Substrate ◽  
The Individual ◽  
Degradation Degree ◽  
Derivatives Of

The effect of exo-D-galacturonanase from carrot on O-acetyl derivatives of pectic acid of variousacetylation degree was studied. Substitution of hydroxyl groups at C(2) and C(3) of D-galactopyranuronic acid units influences the initial rate of degradation, degree of degradation and its maximum rate, the differences being found also in the time of limit degradations of the individual O-acetyl derivatives. Value of the apparent Michaelis constant increases with increase of substitution and value of Vmax changes. O-Acetyl derivatives act as a competitive inhibitor of degradation of D-galacturonan. The extent of the inhibition effect depends on the degree of substitution. The only product of enzymic reaction is D-galactopyranuronic acid, what indicates that no degradation of the terminal substituted unit of O-acetyl derivative of pectic acid takes place. Substitution of hydroxyl groups influences the affinity of the enzyme towards the modified substrate. The results let us presume that hydroxyl groups at C(2) and C(3) of galacturonic unit of pectic acid are essential for formation of the enzyme-substrate complex.

scholarly journals Gene Sequencing and Phylogenetic Analysis: Powerful Tools for an Improved Diagnosis of Fish Mycobacteriosis Caused by Mycobacterium fortuitum Group Members

2021 ◽  
Vol 9 (4) ◽  
pp. 797
Author(s):  
Davide Mugetti ◽  
Mattia Tomasoni ◽  
Paolo Pastorino ◽  
Giuseppe Esposito ◽  
Vasco Menconi ◽  
...  
Keyword(s):  
Phylogenetic Analysis ◽  
Gene Sequencing ◽  
Diagnostic Techniques ◽  
Individual Species ◽  
Identification System ◽  
Mycobacterium Fortuitum ◽  
Biochemical Tests ◽  
Species Determination ◽  
Gene Encoding ◽  
The Individual

The Mycobacterium fortuitum group (MFG) consists of about 15 species of fast-growing nontuberculous mycobacteria (NTM). These globally distributed microorganisms can cause diseases in humans and animals, especially fish. The increase in the number of species belonging to MFG and the diagnostic techniques panel do not allow to clarify their real clinical significance. In this study, biomolecular techniques were adopted for species determination of 130 isolates derived from fish initially identified through biochemical tests as NTM belonging to MFG. Specifically, gene sequencing and phylogenetic analysis were used based on a fragment of the gene encoding the 65 KDa heat shock protein (hsp65). The analyzes made it possible to confirm that all the isolates belong to MFG, allowing to identify the strains at species level. Phylogenetic analysis substantially confirmed what was obtained by gene sequencing, except for six strains; this is probably due to the sequences present in NCBI database. Although the methodology used cannot represent a univocal identification system, this study has allowed us to evaluate its effectiveness as regards the species of MFG. Future studies will be necessary to apply these methods with other gene fragments and to clarify the real pathogenic significance of the individual species of this group of microorganisms.

scholarly journals Aconitum lipo-alkaloids – Semisynthetic Products of the Traditional Medicine

2011 ◽  
Vol 6 (4) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Botond Borcsa ◽  
Dezső Csupor ◽  
Peter Forgo ◽  
Ute Widowitz ◽  
Rudolf Bauer ◽  
...  
Keyword(s):  
Complex Mixture ◽  
Long Chain Fatty Acid ◽  
Diterpene Alkaloids ◽  
Highly Sensitive ◽  
Minor Compounds ◽  
The Individual ◽  
Traditional Processing ◽  
Far Eastern ◽  
Derivatives Of ◽  
General Method

The term lipo-alkaloid is used for C19 aconitane alkaloids containing one or two long-chain fatty acid residues. Lipo-alkaloids are transesterified derivatives of the most toxic and highly effective diester-type diterpene alkaloids, such as aconitine, hypaconitine, mesaconitine. Lipo-alkaloids are native minor compounds of aconite drugs, but their amount significantly increases after traditional processing, which is a general method in the Far Eastern traditional medicinal systems. Analytical works demonstrated that cautious processing (usually boiling) of crude aconite roots decreases the amount of normal diterpene alkaloids and increases the concentration of lipo-alkaloids resulting in the reduction of toxicity of the drugs. Many papers reported that lipo-alkaloids occur as a complex mixture in the drugs, and the isolation of the individual components is extremely difficult. These compounds have been identified using highly sensitive analytical methods (HPLC-MS, NMR), and semisynthetic approaches have been developed to ensure lipo-alkaloids in pure form for pharmacological studies. This review summarizes the structure, chemistry, semisynthesis, analytics and bioactivities of lipo-alkaloids. On the basis of 32 references this is the first comprehensive study on this topic, covering the data of 173 compounds.

scholarly journals Improving weather and climate predictions by training of supermodels

2019 ◽  
Author(s):  
Francine Schevenhoven ◽  
Frank Selten ◽  
Alberto Carrassi ◽  
Noel Keenlyside
Keyword(s):  
Time Derivative ◽  
Learning Rule ◽  
Training Methods ◽  
Model Errors ◽  
Climate Simulations ◽  
Weather And Climate ◽  
Present Context ◽  
Training Schemes ◽  
The Individual ◽  
Derivatives Of

Abstract. Recent studies demonstrate that weather and climate predictions potentially improve by dynamically combining different models into a so called "supermodel". Here we focus on the weighted supermodel – the supermodel's time derivative is a weighted superposition of the time-derivatives of the imperfect models, referred to as weighted supermodeling. A crucial step is to train the weights of the supermodel on the basis of historical observations. Here we apply two different training methods to a supermodel of up to four different versions of the global atmosphere-ocean-land model SPEEDO. The standard version is regarded as truth. The first training method is based on an idea called Cross Pollination in Time (CPT), where models exchange states during the training. The second method is a synchronization based learning rule, originally developed for parameter estimation. We demonstrate that both training methods yield climate simulations and weather predictions of superior quality as compared to the individual model versions. Supermodel predictions also outperform predictions based on the commonly used Multi-Model Ensemble (MME) mean. Furthermore we find evidence that negative weights can improve predictions in cases where model errors do not cancel (for instance all models are warm with respect to the truth). In principle the proposed training schemes are applicable to state-of-the-art models and historical observations. A prime advantage of the proposed training schemes is that in the present context relatively short training periods suffice to find good solutions. Additional work needs to be done to assess the limitations due to incomplete and noisy data, to combine models that are structurally different (different resolution and state representation for instance) and to evaluate cases for which the truth falls outside of the model class.

scholarly journals Flight and Molecular Modeling Study on the Response of Codling Moth, Cydia pomonella (Lepidoptera: Tortricidae) to (E,E)-8,10-Dodecadien-1-ol and Its Geometrical Isomers

2000 ◽  
Vol 55 (11-12) ◽  
pp. 1011-1017 ◽  
Author(s):  
Ashraf El-Sayed ◽  
Ilme Liblikas ◽  
Rikard Unelius
Keyword(s):  
Molecular Modeling ◽  
Cydia Pomonella ◽  
Codling Moth ◽  
Flight Behavior ◽  
Behavioral Activity ◽  
Geometrical Isomers ◽  
Specific Receptors ◽  
Flight Parameters ◽  
The Individual ◽  
Number Of Males

In a previous study we have reported that both (E,Z )-8,10-dodecadienol (E,Z ) and (Z,Z )- 8,10-dodecadienol (Z,Z ) isomers inhibit the attraction of male codling moth, Cydia pomonella L. when added to (E,E)-8,10-dodecadienol (E,E ) while the (E,E)-8,10-dodecadienol (Z,E ) isomer induces slight increase in the number of males attracted to the pheromone source. In the p resent study, we have tested the behavioral activity of the individual geometrical isomers E,Z; Z,E and Z,Z . A few number of codling moth males flew to the Z,E -isomer while the other two isomers (i.e. E,Z and Z,Z ) did not elicit any upwind orientation. Analysis of the flight behavior to the E,E- and Z,E-isomer showed significant differences in most of the flight parameters evaluated. Based on the biological observations and molecular modeling, we suggest that the behavioral activity of the Z,E-isomer is due to presence of specific receptors for this isomer on male antennae and not to its structural resemblance to the E,E-isomer. These results underline the importance of the Z,E-isomer in sex attraction of male codling moth.

Gas-chromatographic determination of nanogram amounts of enantiomers of nortilidine, a main metabolite of tilidine, in biological specimens.

1978 ◽  
Vol 24 (4) ◽  
pp. 692-697 ◽  
Author(s):  
H Hengy ◽  
K O Vollmer ◽  
V Gladigau
Keyword(s):  
Intravenous Administration ◽  
Chromatographic Determination ◽  
Optical Isomers ◽  
Sensitive Detector ◽  
Main Metabolite ◽  
Chiral Reagent ◽  
The Individual ◽  
Derivatives Of ◽  
Sensitive Method

Abstract We report a specific and sensitive method for determination of the individual optical isomers of nortilidine, a main metabolite of tilidine, with the aid of a nitrogen-sensitive detector. With N-trifluoroacetyl-L-leucyl chloride as chiral reagent, the diastereomeric derivatives of the nortilidine enantiomers could be separated and quantified in the nanogram range. Under these conditions, the enantiomers of bisnortilidine, another main metabolite of tilidine, were also separated. Investigations in rats with the enantiomers of tilidine and nortilidine indicated that no racemization occurs during N-demethylation in the organism. After oral and intravenous administration of 50 mg of tilidine.HCI to a human volunteer, identical concentrations of nortilidine enantiomers were found in the plasma.

A Review of the Literature as to the Present Possibilities and Limitations in Estimating the Time of Death

1976 ◽  
Vol 16 (4) ◽  
pp. 269-276 ◽  
Author(s):  
R. Van Den Oever
Keyword(s):  
Forensic Medicine ◽  
Large Error ◽  
Time Of Death ◽  
Post Mortem ◽  
Review Of The Literature ◽  
Biochemical Tests ◽  
Post Mortem Interval ◽  
Suitable Combination ◽  
Exact Moment ◽  
The Individual

Determining the exact moment of death in medicolegal cases is not possible since post-mortem changes of the human body are variable and often misjudged. The most reliable physical and biochemical methods of estimating the post-mortem interval are reviewed and the author tries to find out why, in spite of all the previous studies, which have often given good results, the individual methods are neither popular nor practical in routine forensic medicine cases. For greater accuracy in estimating the time of death further investigation should be carried out to find a suitable combination of some physical and biochemical tests complementary to the data produced by each method and preventing the rather large error range of each individual test.

A new classification of solvents based on chemometric empirical scale of parameters

1990 ◽  
Vol 55 (3) ◽  
pp. 644-652 ◽  
Author(s):  
Oldřich Pytela
Keyword(s):  
Causal Relation ◽  
Carbon Disulphide ◽  
Dimensional Space ◽  
Three Dimensional ◽  
Solvent Polarity ◽  
Clustering Methods ◽  
Hexamethylphosphoric Triamide ◽  
Centroid Method ◽  
The Individual

The paper presents a classification of 51 solvents based on clustering in three-dimensional space formed by the empirical scale of PAC, PBC, and PPC parameters designed for interpretation of solvent effect on a model with cross-terms. For the classification used are the clustering methods of the nearest neighbour, of the furthest neighbour, of average bond, and the centroid method. As a result, the solvents have been divided into 8 classes denoted as: I - nonpolar-inert solvents (aliphatic hydrocarbons), IIp - nonpolar-polarizable (aromatic hydrocarbons, tetrachloromethane, carbon disulphide), IIb - nonpolar-basic (ethers, triethylamine), IIIp - little polar-polarizable (aliphatic halogen derivatives, substituted benzenes with heteroatom-containing substituents), IIIb - little polar-basic (cyclic ethers, ketones, esters, pyridine), IVa - polar-aprotic (acetanhydride, dialkylamides, acetonitrile, nitromethane, dimethyl sulfoxide, sulfolane), IVp - polar-protic (alcohols, acetic acid), and V - exceptional solvents (water, formamide, glycol, hexamethylphosphoric triamide). The information content of the individual parameters used for the classification has been determined. The classification is based primarily on solvent polarity/acidity (PAC), less on polarity/basicity (PBC), and the least on polarity/polarizability (PPC). Causal relation between chemical structure of solvent and its effect on the process taking place therein has been established.

scholarly journals Halorubrum ezzemoulense sp. nov., a halophilic archaeon isolated from Ezzemoul sabkha, Algeria

2006 ◽  
Vol 56 (7) ◽  
pp. 1583-1588 ◽  
Author(s):  
Karima Kharroub ◽  
Teresa Quesada ◽  
Raquel Ferrer ◽  
Susana Fuentes ◽  
Margarita Aguilera ◽  
...  
Keyword(s):  
Dna Hybridization ◽  
Genomic Dna ◽  
Type Strain ◽  
Rrna Gene ◽  
Halophilic Archaeon ◽  
16S Rrna Gene Sequences ◽  
Biochemical Tests ◽  
Phenotypic Differentiation ◽  
Extremely Halophilic Archaeon ◽  
Derivatives Of

A novel extremely halophilic archaeon was isolated from Ezzemoul sabkha, Algeria. The strain, designated 5.1T, was neutrophilic, motile and Gram-negative. At least 15 % (w/v) NaCl was required for growth. The isolate grew at pH 6.5–9.0, with optimum growth at pH 7.0–7.5. Mg2+ was required for growth. Polar lipids were C20C20 derivatives of phosphatidylglycerol and phosphatidylglycerol phosphate methyl ester, and phosphatidylglycerol sulfate and sulfated diglycosyl diether. The genomic DNA G+C content of strain 5.1T was 61.9 mol% (T m). Phylogenetic analysis based on comparison of 16S rRNA gene sequences revealed that strain 5.1T clustered with Halorubrum species. The results of DNA–DNA hybridization and biochemical tests allowed genotypic and phenotypic differentiation of strain 5.1T from other Halorubrum species. The name Halorubrum ezzemoulense sp. nov. (type strain 5.1T=CECT 7099T=DSM 17463T) is proposed.

Extended use of receiver groups: Theory, synthetic example, and noise considerations

Geophysics ◽  
2020 ◽  
Vol 85 (6) ◽  
pp. P53-P66
Author(s):  
Kjetil E. Haavik
Keyword(s):  
Noise Level ◽  
Signal To Noise Ratio ◽  
Random Noise ◽  
Higher Order ◽  
Sinc Interpolation ◽  
Seismic Acquisition ◽  
Multichannel Sampling ◽  
The Individual ◽  
Derivatives Of ◽  
The Ideal

Receiver grouping is commonly used in marine towed-streamer seismic acquisition. Measurements from several receivers in a group are stacked to increase the signal-to-noise ratio of the resulting data and form an analog spatial antialiasing filter. I propose a method for extracting inline derivatives of the wavefield as additional measurements from the groups. This is achieved by multiplying the signal from the individual receivers in a group with predefined weights that corresponds to a finite-difference (FD) operator. The inline derivative(s) makes it possible to use multichannel sampling theorems to reconstruct the signal on a denser grid. Extraction of FD data from clusters of receivers is not a new concept, but I find that, by using the geometry of conventional streamer groups, it is possible to obtain FD data which are well suited for multichannel interpolation. The key to finding suitable FD operators is to recognize that it is not the ideal differentiation response we seek, but the impulse response of the group multiplied with the ideal differentiation response. Furthermore, under a Gaussian noise assumption, I derive formulas for the resulting noise level from sinc and higher order sinc interpolations. I find that the random noise level in the reconstructed data, when using higher order sinc interpolation, is expected to be higher than when using conventional sinc interpolation and will vary with respect to the distance from the original sampling points. The statistical analysis shows that it is beneficial to find FD operators with as small an [Formula: see text] norm as possible. A synthetic example shows that the proposed method of extracting FD operators and subsequent interpolation works very well. I foresee that the proposed method can be used to reduce the density of receivers (hydrophones or geophones) when designing new streamers or with existing equipment to improve the inline sampling.

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