scholarly journals Monitoring Wnt Protein Acylation Using an In Vitro Cyclo-Addition Reaction

2016 ◽  
pp. 11-16
Author(s):  
Rubina Tuladhar ◽  
Nageswari Yarravarapu ◽  
Lawrence Lum
Keyword(s):  
Addition Reaction ◽  
Protein Acylation

scholarly journals Synthesis, in vitro and in silico Studies of Naphthalene Pyrazoline Prop-2-en-1-one Derivatives

2020 ◽  
Vol 32 (8) ◽  
pp. 1849-1856
Author(s):  
B. Prabha ◽  
C. Raja ◽  
S. Nathiya ◽  
M.R. Ezhilarasi
Keyword(s):  
Binding Affinity ◽  
Addition Reaction ◽  
Condensation Reaction ◽  
Docking Studies ◽  
High Drug ◽  
In Silico Studies ◽  
Drug Score ◽  
The Michael Addition ◽  
High Inhibition

The synthesized new naphthalene pyrazoline prop-2-en-1-one derivatives (NDPP 1-8) were obtained by the Michael addition reaction of ethyl propanoate, hydrazine hydrate with NPD as a multicomponent scaffold. (E)-1-(naphthalen-3-yl)-3-phenylprop-2-en-1-one (NPD) was formed from 2-acetyl naphthalene and substituted aldehyde via Claisen-Schmidt condensation reaction. The NDPP skeleton structures were confirmed by infrared, 1H & 13C NMR spectral data and elemental analysis. The structure of NDPP compounds was subjected to molecular docking and ADME studies. The result of ADME prediction, compound NDPP 2, which contains electron withdrawing -Cl group has high drug-likeness value 4.21 than the compounds NDPP 4 and 7 which had electron donating CH3 and OCH3 group shows the drug-likeness value 2.62. The NDPP 2 also has high drug score 0.63 than NDPP 4 and NDPP 7 have drug score 0.60 and 0.69, respectively. Docking studies shows that compound NDPP 5 which also contain electron withdrawing NO2 group has good binding affinity value -8.8 Kcal/mol were docked with 1UAG protein. These compounds showed good drug-likeness value 2.25 and drug score 0.65. in vitro Studies have a high inhibition value for the same NO2 substituted derivative. All the compounds have higher binding affinity value than standards binding affinity value.

scholarly journals A Comparative Study on Accuracy and Reproducibility of Alginate and Addition Reaction Silicone as an Impression Materials.

2014 ◽  
Vol 3 (2) ◽  
pp. 28-33
Author(s):  
Shakila Fatema ◽  
Sheikh Md Shahriar Quader ◽  
Mohammad Shamsuzzaman ◽  
Mirza Md Arifur Rahman ◽  
Nasima Khan
Keyword(s):  
Addition Reaction ◽  
In Vitro Study ◽  
Dimensional Accuracy ◽  
Horizontal Line ◽  
Impression Material ◽  
Dimensional Changes ◽  
Impression Materials ◽  
Study Results ◽  
Surface Detail

Background: To achieve accuracy and exact reproduction of prosthesis, choosing a perfect impression material is essential. Especially to make the prosthesis as accurately as possible, impression material should possess some essential properties, like; minimum dimensional changes, good flow ability and easy removal. Purpose: The aim of this study was to evaluate the accuracy and surface detail reproduction of Alginate and Addition Reaction Silicone as an impression materials. Method: This is an experimental in vitro study. In this study Impression by Alginate and Addition Reaction Silicone were made using a round stainless steel test block with three horizontal lines and two vertical lines. The horizontal lines were used for evaluating the surface detail reproduction, and vertical lines were provided for the dimensional accuracy. For dimensional accuracy the length of the middle horizontal line in between vertical lines and the distance between the top and bottom horizontal line was measured using travelling microscope. And for surface detail reproduction three horizontal line of one segment were observed under stereomicroscope. Result: According to study results Addition Reaction Silicone is better than Alginate regarding quality of impression. Conclusion: In comparison to Alginate, Addition Reaction Silicone might have better performance about accuracy and surface detail reproduction. DOI: http://dx.doi.org/10.3329/updcj.v3i2.17996 Update Dent. Coll. j: 2013; 3 (2): 28-33

An in vitro study of a surface wetting agent for addition reaction silicone impressions

1994 ◽  
Vol 71 (4) ◽  
pp. 390-393 ◽  
Author(s):  
P. Brett Robinson ◽  
Stephen M. Dunne ◽  
Brian J. Millar
Keyword(s):  
Addition Reaction ◽  
In Vitro Study ◽  
Vitro Study ◽  
Wetting Agent ◽  
Surface Wetting

scholarly journals Synthesis and Antimalarial Activity of 7-Chloro-4-(4-(2-(Oxo, Hydroxyl & Fluoro-2-1 (4-Phenyl)Ethyl)Piperazin-1-yl)Quinoline Derivatives

2021 ◽  
Vol 12 (6) ◽  
pp. 7957-7971
Keyword(s):  
Nucleophilic Addition ◽  
Addition Reaction ◽  
Antimalarial Activity ◽  
Quinoline Derivatives ◽  
Good Activity ◽  
Standard Drug ◽  
Falciparum Strain ◽  
Phenacyl Bromides ◽  
Nucleophilic Addition Reaction

Since these days, microbes are resistant to the drugs available in the market, which has caused an alarming impact on society. 18 compounds in a series of 7-chloro-4-(piperazin-1-yl)quinoline derivatives were synthesized by nucleophilic addition reaction of piperazine with 4,7-dichloroquinoline followed by phenacyl bromides addition to heteroaryl piperazine and then reduction and fluorination. All 18 compounds were evaluated in vitro for their antimalarial activity against plasmodium falciparum strain. Although 12 compounds showed good activity, compound 3c was found to be more potent than standard drug Quinine having MIC 0.18 μg/ mL. On the other hand, 3d, 3e, 5a, and 5f were found to be equipotent (MIC 0.26 μg/ mL) to the standard drug.

scholarly journals Evidence that coated vesicles transport acetylcholine receptors to the surface membrane of chick myotubes.

1984 ◽  
Vol 98 (2) ◽  
pp. 498-506 ◽  
Author(s):  
S Bursztajn ◽  
G D Fischbach
Keyword(s):  
Acetylcholine Receptors ◽  
Prolonged Exposure ◽  
Addition Reaction ◽  
Surface Membrane ◽  
Coated Vesicles ◽  
Intact Cells ◽  
Saline Extract ◽  
Permeabilized Cells ◽  
Alpha Bungarotoxin

Coated vesicles are present in the myoplasm of embryonic chick myotubes grown in vitro. They are most numerous beneath regions of the surface membrane that contain a high density of acetylcholine receptors (AChR). Prolonged exposure of myotubes to saline extract of chick brain increases the number of intracellular AChR and the number of coated vesicles. This suggests that coated vesicles contain AChR, and this hypothesis was tested with horseradish peroxidase-alpha-bungarotoxin (HRP-alpha BTX) conjugates. The conjugates enter saponin-permeabilized cells and, as judged by the inhibition of [125I] alpha BTX binding, they label the entire intracellular AChR pool. Approximately 50% of the coated vesicles contained HRP-alpha BTX reaction product. In addition, reaction product was detected in Golgi cisternae and along membranes that bound a subsurface tubulovesicular network. The majority of labeled vesicles are probably involved in exocytosis rather than endocytosis of AChR because very few coated vesicles were labeled when HRP-alpha BTX was added to the medium bathing intact cells. Moreover, inhibition of protein synthesis with puromycin resulted in a large decrease in the number of labeled vesicles. These results suggest that a subpopulation of coated vesicles ferry newly synthesized AChR to the cell surface.

scholarly journals A Study on Antitumor Effect of 1,3,4-Thiadiazole Derivatives in Prostate and Breast Cancer Cell Lines (In Vitro)

2017 ◽  
Author(s):  
Firas Hassan ◽  
Nany Hairunisa ◽  
Salam A. Mohammed ◽  
Emad Yousif
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Addition Reaction ◽  
Breast Cancer Cell Lines ◽  
Human Prostate Cancer ◽  
Malignant Cells ◽  
Thiadiazole Derivative ◽  
Different Types ◽  
Before And After

5-(4-aminophenyl )-2-amino -1,3,4-thiadiazole was prepared by reaction of Thiosemicarbazide with 4-amino benzoic acid under reflux condition for 7 hours. The compound which has been synthesized successfully was subjected to addition reaction with 4-(Dimethylamino) benzaldehyde under reflux condition for 6 hours to synthesize Schiff bases. These compounds was characterized by using FTIR) and evaluated for their anticancer activity. The effect of (1, 3, 4-thiadiazole derivative) on the activity of malignant cells was studied by using different types of cell lines [Breast cancer, and human prostate cancer]. And was used the Electron microscope to show that the effect of the derivative on the cancer cells before and after 3 days of the injection time. It was found that the Schiff base of thiadiazole-1,3,4-(Dimethylamino)benzylidineamino]- [4-2-phenyl]amino was effective in reducing the size and density of malignant cells. That of 46.7 while in breast ) 145(DUprostate for growth inhibition produce of equal 85.9 µg/ml.

scholarly journals Noncovalent Complexation of Amphotericin B with Poly(β-Amino Ester) Derivates for Treatment of C. Neoformans Infection

Polymers ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 270 ◽  
Author(s):  
Yang Yu ◽  
Li Peng ◽  
Guojian Liao ◽  
Zhangbao Chen ◽  
Chong Li
Keyword(s):  
Amphotericin B ◽  
Addition Reaction ◽  
Noncovalent Complex ◽  
Drug Loading ◽  
Amino Ester ◽  
Poly Ethylene Glycol ◽  
Improve Treatment ◽  
Michael Type Addition ◽  
Poly Ethylene

Our goal was to improve treatment outcomes for C. neoformans infection by designing nanocarriers that enhance drug-encapsulating capacity and stability. Thus, a noncovalent complex of methoxy poly(ethylene glycol)-poly(lactide)-poly(β-amino ester) (MPEG-PLA-PAE) and amphotericin B (AMB) was developed and characterized. The MPEG-PLA-PAE copolymer was synthesized by a Michael-type addition reaction; the copolymer was then used to prepare the AMB-loaded nanocomplex. AMB was in a highly aggregated state within complex cores. A high encapsulation efficiency (>90%) and stability of the AMB-loaded nanocomplex were obtained via electrostatic interaction between AMB and PAE blocks. This nanocomplex retained drug activity against C. neoformans in vitro. Compared with micellar AMB, the AMB nanocomplex was more efficient in terms of reducing C. neoformans burden in lungs, liver, and spleen, based on its improved biodistribution. The AMB/MPEG-PLA-PAE complex with enhanced drug-loading capacity and stability can serve as a platform for effective treatment of C. neoformans infection.

1-(4-Cyclopentylphenyl)piperazine and its 4-substituted derivatives; Synthesis and biological screening

1987 ◽  
Vol 52 (7) ◽  
pp. 1834-1840 ◽  
Author(s):  
Zdeněk Vejdělek ◽  
Miroslav Protiva
Keyword(s):  
Antimicrobial Activity ◽  
Benzyl Chloride ◽  
Addition Reaction ◽  
Anthelmintic Activity ◽  
Ethyl Formate ◽  
Lithium Aluminium Hydride ◽  
Biological Screening ◽  
Acyl Chlorides ◽  
Lithium Aluminium

Heating the hydrochlorides of 4-cyclopentylaniline and diethanolamine to 250 °C gave 1-(4-cyclopentylphenyl)piperazine (I). Acylation of I with ethyl formate and the corresponding acyl chlorides gave the amides II, VI, and VII which were reduced with lithium aluminium hydride to the piperazines III, VIII, and IX. Treatment of I with benzyl chloride and with 4-chloro-1-(4-fluorophenyl)butan-1-one under different conditions led to compounds IX and XI. Addition reaction of I to 1,2-epoxybutane resulted in the amino alcohol V. The products showed marginal tranquillizing activity (especially compound VIII), some antimicrobial activity in vitro and some anthelmintic activity.

scholarly journals Hemostatic Patches Based on Crosslinked Chitosan Films Applied in Interventional Procedures

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2402
Author(s):  
Moon Hyun Lee ◽  
Dae Ryeong Lee ◽  
Joon Woo Chon ◽  
Dong June Chung
Keyword(s):  
Blood Clotting ◽  
Addition Reaction ◽  
Coupling Reaction ◽  
Biological Properties ◽  
Activated Partial Thromboplastin Time ◽  
Cytotoxicity Test ◽  
Diphenyltetrazolium Bromide ◽  
Nucleophilic Addition Reaction ◽  
Crosslinked Chitosan

In this study, we manufactured biocompatible hemostatic crosslinked chitosan (CS) patches and analyzed their physicochemical and biological properties for femoral arterial puncture applications. CS is a representative hemostatic material but has some drawbacks, such as swelling, shrinkage, and brittleness. Thus, it was crosslinked via a 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide (EDC)/N-hydroxysuccinimide (NHS) coupling reaction and a nucleophilic addition reaction with citric acid (CA), glutaraldehyde (GTA), and genipin (GP) to remedy its shortcomings. The CSCA (crosslinked CS with CA/EDC), CSGTA (crosslinked CS with GTA), and CSG (crosslinked CS with GP) films showed low swelling degrees and good mechanical properties (excluding CSCA) compared with those of neat CS films. Additionally, every crosslinked CS film coated with thrombin (TB-CS) showed enhanced hemostatic ability in the whole blood clotting and activated partial thromboplastin time tests. Furthermore, the CSCA, CSGTA, and CSGP were nontoxic in an in vitro cell cytotoxicity test (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide assay) using L-929 mouse fibroblasts cells.

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