scholarly journals Synthesis of Some New 2-Methyl -1,4-benzothiazine-3(1H)- one Derivatives as Potential Vasodilators

2004 ◽  
Vol 1 (4) ◽  
pp. 206-210 ◽  
Author(s):  
M. B. Deshmukh ◽  
A. R. Mulik ◽  
Savita Dhongade-Desai
Keyword(s):  
Blood Flow ◽  
Biological Activities ◽  
Local Environment ◽  
Internal Diameter ◽  
Fresh Blood ◽  
Software Application ◽  
Wide Range ◽  
Normal Metabolism ◽  
Cardiac Disorders ◽  
The Relationship

The increase in the internal diameter of a blood vessel that results from relaxation of smooth muscle within the wall of the vessel is vasodilation. This causes an increase in blood flow and a decrease in systemic vascular resistance. Some substances produced by tissue deprived of fresh blood seem to be responsible for the dilation. Many products of metabolism bring about the action, CO2and acids are among them. Dilation of vessels is necessary to restore local environment of tissues and normal metabolism. It may prove to be potential in the treatment of different cardiac disorders like atherosclerosis, where, the blood vessels are narrowed due to deposition of plaque of substances like cholesterol etc. 1,4-benzothiazines have been reported to possess wide range of pharmacological and biological activities. Here, we report the synthesis and biological activity of some new arylidenehydrazino-(1H)-1,4-benzothiazines. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. The relationship between structure and different biological activities was studied and it was found that the arylidenehydrazino-(1H)-1,4-benzothiazines are expected to be potential vasodilators.

Measurements of Hemodialysis Catheter Blood Flow in Vivo

2002 ◽  
Vol 25 (4) ◽  
pp. 276-280 ◽  
Author(s):  
Z. J. Twardowski ◽  
J. D. Haynie
Keyword(s):  
Blood Flow ◽  
Average Length ◽  
Internal Diameter ◽  
Hemodialysis Catheter ◽  
Blood Flows ◽  
Catheter Design ◽  
Poiseuille’S Equation ◽  
Different Diameters ◽  
The Relationship

The relationship between the blood flow and inflow and outflow pressures was determined in PermCath, dual lumen catheters during regular hemodialyses in vivo in eight patients with average hematocrit of 38%. From the luer lock connector the catheters had an average length of 32 cm to the outflow tip and 30 cm to the inflow tip. The catheters had an internal diameter of 0.2 cm and were straight before implantation. Dialyses were performed on Fresenius 2008 D or E machines with ReadySet™ blood lines with an 8 mm ID pump segment and a noncollapsible arterial chamber. Pressures and blood flows were measured at pump speeds from 50 to 500 ml/min in increments of 50 ml/min with lines in normal configuration. Blood flow was measured continuously using ultrasound. The correlations between pressures and flows are not linear. The best correlations are according to the Stirling model of exponential growth category equation. Inflow pressure = -9.07–0.4865*(exp(0.0020*blood flow)-1)/0.0020 Outflow pressure = -28.14+0.5002*(exp(0.0015*blood flow)-1/0.0015 Based on these results and Poiseuille's equation a table was developed for the optimal relationship between catheter length and diameter to achieve standardized (average, low and high) blood flows regardless of the lengths of the catheters. The diameter/length relationships are based on theoretical considerations. Because resistances depend on the material and shape of the tubing, the actual measurements of flow/pressure relationships should be done once tubings of different diameters are manufactured, and final catheter design has to be based on these measurements.

Peripheral venous catecholamines versus adrenal secretory rates after brain stem stimulation in cats

1986 ◽  
Vol 251 (1) ◽  
pp. E14-E20 ◽  
Author(s):  
D. A. Bereiter ◽  
W. C. Engeland ◽  
D. S. Gann
Keyword(s):  
Blood Flow ◽  
Electrical Stimulation ◽  
Brain Stem ◽  
Catecholamine Secretion ◽  
Wide Range ◽  
Before And After ◽  
Alpha Chloralose ◽  
The Relationship ◽  
Adrenal Secretion ◽  
Catecholamine Concentration

The relationship between adrenal catecholamine secretion and peripheral venous catecholamine concentration was assessed in samples collected before and after brief (15-s) periods of brain stem electrical stimulation in cats anesthetized with alpha-chloralose-urethan. Adrenal blood flow from the left lumboadrenal vein averaged 0.75 +/- 0.05 ml/min (means +/- SE, n = 56). Peripheral norepinephrine (NE) concentration (1.19 +/- 0.07 ng/ml) was not well correlated with adrenal NE secretion (38.18 +/- 3.99 ng/min) before stimulation (r = 0.334, P less than 0.025). Although brain stem sites that evoked large increases in adrenal NE secretion often caused an increase in peripheral NE, sites that evoked significant decreases in adrenal NE secretion were not accompanied by decreases in peripheral NE. Peripheral epinephrine (E) concentration (0.11 +/- 0.01 ng/ml) was well correlated with adrenal E secretion (23.72 +/- 2.33 ng/min) before stimulation (r = 0.468, P less than 0.001). Brain stem stimulation-evoked changes in adrenal E secretion were generally reflected in changes of peripheral E concentration, although many exceptions were seen. Peripheral dopamine (DA) concentration (0.23 +/- 0.02 ng/ml) was well correlated with adrenal DA secretion (0.94 +/- 0.11 ng/min) before stimulation (r = 0.505, P less than 0.001). However, stimulus-evoked changes in adrenal DA secretion were not reflected in changes of peripheral DA concentration. The data indicate that, whereas brief periods of brain stem stimulation evoke a wide range of adrenal secretory responses, peripheral catecholamine responses best reflected adrenal secretion only when large increases in adrenal secretion were evoked and were poor indicators of decreased adrenal catecholamine secretion.(ABSTRACT TRUNCATED AT 250 WORDS)

scholarly journals Synthesis and QSAR Study of (4-Oxo-3-aryl-3,4-dihydro-quinazolin-2-ylsulfanyl)-propionic Acid arylidene/aryl-ethylidene-hydrazides via Microwave Assisted Solvent Free Reations

2004 ◽  
Vol 1 (2) ◽  
pp. 115-126
Author(s):  
M. B. Deshmukh ◽  
Savita Dhongade (Desai)
Keyword(s):  
Biological Activities ◽  
Hdl Cholesterol ◽  
Aromatic Aldehydes ◽  
Solvent Free ◽  
Qsar Study ◽  
Software Application ◽  
Microwave Assisted ◽  
The Relationship ◽  
Derivatives Of ◽  
Microwave Assisted Method

In the present work,s-alkylated derivatives of thio-quinazolinone were obtained using Methyl 2-chloro propionate via a solvent-free microwave-assisted method. The alkylated thio quinazolinones were further sequentially condensed with hydrazine hydrate and different aromatic aldehydes to get the hydrazides, which were studied for QSAR. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. . The relationship between structure and different biological activities was studied and the different derivatives were recommended for the screening of some specific activities like anti-tuberculosic, anti-mycobacterial & HDL cholesterol increasing activities.

scholarly journals RETENTION BEHAVIOR AND BIOLOGICAL ACTIVITY OF N-SUBSTITUTED-2-PHENYLACETAMIDE DERIVATES

2014 ◽  
Vol 5 (1) ◽  
Author(s):  
Đenđi Vaštag ◽  
Suzana Apostolov ◽  
Borko Matijević ◽  
Jelena Nakomčić ◽  
Aleksandar Marinković
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Biological Properties ◽  
Reversed Phase ◽  
Chromatographic Retention ◽  
Wide Range ◽  
Structure Retention ◽  
The Mathematical Model ◽  
The Relationship ◽  
Layer Chromatography

Phenylacetamide derivatives are a group of compounds that exhibit a wide range of biological activities as analgetic, anticonvulsant, pesticide, cytostatic. It is well known that the biological activity and the field of activity of the substance are greatly dependent on its physical, chemical and structural properties. In this paper, we applied QSRR analysis (Quantitative Structure Retention Relationships), which is based on the prediction of biological properties of compounds based on their chromatographic retention behaviors. To that end, retention constants of investigated N-substituted-2-phenylacetamide were determined by reversed phase thin-layer chromatography, (HPTLC RP18 F254s) in the presence of different volume fractions of n-propanol and tetrahydrofuran. The resulting data were correlated with molecular descriptors determined in different ways in order to establish the mathematical model that describes the relationship between retention properties and biological activities of investigated phenylacetamides.

Copper-Catalyzed Azide-Alkyne Cycloaddition (CuAAC)-Mediated Macrocyclization of Peptides: Impact on Conformation and Biological Activity

2018 ◽  
Vol 18 (7) ◽  
pp. 591-610 ◽  
Author(s):  
Chiara Testa ◽  
Anna Maria Papini ◽  
Michael Chorev ◽  
Paolo Rovero
Keyword(s):  
Enzymatic Degradation ◽  
Bioactive Peptides ◽  
Click Reaction ◽  
Biological Activities ◽  
Structural Diversity ◽  
Conformational Space ◽  
Widespread Application ◽  
Wide Range ◽  
The Relationship ◽  
State Of Art

The long-lasting impetus to design novel modes of macrocyclization, and their implementation into a wide range of bioactive peptides, originates from their contributions to the restriction of conformational space and the stabilization of preferential bioactive conformations that support higher efficacy and binding affinity to cognate macromolecular targets, improved specificity and lowering susceptibility to enzymatic degradation processes. Introducing CuI-catalyzed azide-alkyne cycloaddition (CuAAC), a prototypical click reaction, to the field of peptide sciences as a bio-orthogonal reaction that generates a disubstituted-[1,2,3]triazol-1-yl moiety as a pseudopeptidic bond that is peptidomimetic in nature, paved the way to its widespread application as a new and promising mode of macrocyclization. This review presents the state-of-art of CuAAC-mediated macrocyclization as it applies to an expansive range of bioactive peptides and explores the relationship among the structural diversity of CuAACmediated cyclizations, biological activities and conformations.

scholarly journals Synthesis and QSAR Study of Some HDL Cholesterol Increasing Quinazolinone Derivatives

2004 ◽  
Vol 1 (1) ◽  
pp. 17-31 ◽  
Author(s):  
M. B. Deshmukh ◽  
Savita Dhongade (Desai)
Keyword(s):  
Biological Activities ◽  
Alkylating Agents ◽  
Hdl Cholesterol ◽  
Aromatic Aldehydes ◽  
Qsar Study ◽  
Software Application ◽  
Quinazolinone Derivatives ◽  
The Relationship ◽  
Derivatives Of ◽  
Microwave Assisted Method

We describe here an easy and efficient method to obtainS-alkylated derivatives of thio-quinazolinone using different alkylating agents via a solvent-free microwave-assisted method. The alkylated thio quinazolinones were further sequentially condensed with hydrazine hydrate and different aromatic aldehydes to get the hydrazones, which were studied for QSAR. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. The relationship between structure and different biological activities was studied and the different derivatives were recommended for the screening of some specific activities like anti-tuberculosic, anti-mycobacterial and HDL cholesterol increasing activities.

Ventilatory threshold is related to walking tolerance in patients with intermittent claudication

VASA ◽  
2012 ◽  
Vol 41 (4) ◽  
pp. 275-281 ◽  
Author(s):  
da Rocha Chehuen ◽  
G. Cucato ◽  
P. dos Anjos Souza Barbosa ◽  
A. R. Costa ◽  
M. Ritti-Dias ◽  
...  
Keyword(s):  
Blood Flow ◽  
Oxygen Uptake ◽  
Intermittent Claudication ◽  
Lower Limb ◽  
Ventilatory Threshold ◽  
Reactive Hyperemia ◽  
Ankle Brachial Index ◽  
Metabolic Parameters ◽  
Walking Distance ◽  
The Relationship

Background: This study assessed the relationship between lower limb hemodynamics and metabolic parameters with walking tolerance in patients with intermittent claudication (IC). Patients and methods: Resting ankle-brachial index (ABI), baseline blood flow (BF), BF response to reactive hyperemia (BFRH), oxygen uptake (VO2), initial claudication distance (ICD) and total walking distance (TWD) were measured in 28 IC patients. Pearson and Spearman correlations were calculated. Results: ABI, baseline BF and BF response to RH did not correlate with ICD or TWD. VO2 at first ventilatory threshold and VO2peak were significantly and positively correlated with ICD (r = 0.41 and 0.54, respectively) and TWD (r = 0.65 and 0.71, respectively). Conclusions: VO2peak and VO2 at first ventilatory threshold, but not ABI, baseline BF and BFHR were associated with walking tolerance in IC patients. These results suggest that VO2 at first ventilatory threshold may be useful to evaluate walking tolerance and improvements in IC patients.

The Problem of Identifying and Modeling the Relationship between Monetary Factor and Inflation in the Russian Economy

2008 ◽  
pp. 61-76
Author(s):  
A. Porshakov ◽  
A. Ponomarenko
Keyword(s):  
Money Supply ◽  
Money Demand ◽  
Russian Economy ◽  
Long Run ◽  
Complex Approach ◽  
Wide Range ◽  
Long Time ◽  
The Relationship ◽  
Supply Side Factors

The role of monetary factor in generating inflationary processes in Russia has stimulated various debates in social and scientific circles for a relatively long time. The authors show that identification of the specificity of relationship between money and inflation requires a complex approach based on statistical modeling and involving a wide range of indicators relevant for the price changes in the economy. As a result a model of inflation for Russia implying the decomposition of inflation dynamics into demand-side and supply-side factors is suggested. The main conclusion drawn is that during the recent years the volume of inflationary pressures in the Russian economy has been determined by the deviation of money supply from money demand, rather than by money supply alone. At the same time, monetary factor has a long-run spread over time impact on inflation.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Synthesis, Characterization and Antiproliferative Activity Assessment of a Novel 1H-5-mercapto-1,2,4 Triazole Derivative

2017 ◽  
Vol 68 (4) ◽  
pp. 745-747 ◽  
Author(s):  
Marius Mioc ◽  
Sorin Avram ◽  
Vasile Bercean ◽  
Mihaela Balan Porcarasu ◽  
Codruta Soica ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Vascular Endothelial ◽  
Triazole Derivative ◽  
Activity Assessment ◽  
Wide Range ◽  
Specific Receptors ◽  
Endothelial Growth Factor ◽  
Selection Of

Angiogenesis plays an important function in tumor proliferation, one of the main angiogenic promoters being the vascular endothelial growth factor (VEGF) which activates specific receptors, particularly VEGFR-2. Thus, VEGFR-2 has become an essential therapeutic target in the development of new antitumor drugs. 1,2,4-triazoles show a wide range of biological activities, including antitumor effect, which was documented by numerous reports. In the current study the selection of 5-mercapto-1,2,4-triazole structure (1H-3-styryl-5-benzylidenehydrazino-carbonyl-methylsulfanil-1,2,4-triazole, Tz3a.7) was conducted based on molecular docking that emphasized it as suitable ligand for VEGFR-2 and EGFR1 receptors. Compound Tz3a.7 was synthesized and physicochemically and biologically evaluated thus revealing a moderate antiproliferative activity against breast cancer cell line MDA-MB-231.

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