ChemInform Abstract: 4-Aryl-1-piperazinylalkyl Derivatives of 1,2,3,4-Tetrahydro-β- carboline Ring System. Synthesis and Preliminary in vivo Studies.

ChemInform ◽  
2010 ◽  
Vol 28 (15) ◽  
pp. no-no
Author(s):  
M. T. CEGLA ◽  
J. BOKSA ◽  
E. CHOJNACKA-WOJCIK ◽  
S. MISZTAL
Keyword(s):  
Ring System ◽  
In Vivo Studies ◽  
System Synthesis ◽  
Derivatives Of

Two in one: bifunctional derivatives of trolox acting as antimalarial and antioxidant agents

2020 ◽  
Vol 12 (20) ◽  
pp. 1845-1854
Author(s):  
Florence Souard ◽  
Edwige Nicolle ◽  
Delphine Cressend ◽  
Alexis Valentin ◽  
Ahcène Boumendjel
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
In Vivo Studies ◽  
Chemical Libraries ◽  
Falciparum Strain ◽  
Antioxidant Agents ◽  
One Step ◽  
Set Up ◽  
Derivatives Of

Background: The aim of the present work was to set-up compounds that are able to act simultaneously as antimalarial and antioxidants. Trolox, a known antioxidant was chosen as a core structure to ensure the antioxidant activity and contribute to antiplasmodial effect. Results: Ten compounds were prepared in one step and evaluated on chloroquino-sensitive (3D7) and chloroquino-resistant (FcB1) strains of Plasmodium falciparum. The most active compound (3d) shows antiplasmodial activity in the range of chloroquine against chloroquino-sensitive and chloroquino-resistant P. falciparum strain. The antioxidant activity of (3d) was conducted through four tests and was found to be more potent than trolox itself and L-ascorbic acid. Conclusion: Compound (3d) can be considered as an excellent lead molecule for further in vivo studies. This study paves the way for building large chemical libraries to be investigated in the field of malaria.

scholarly journals Possible Mechanisms Involved in the Vasorelaxant Effect Produced by Anorexigenic Drugs in Rat Aortic Rings

2019 ◽  
Vol 7 (3) ◽  
pp. 39 ◽  
Author(s):  
Daniela García-Alonso ◽  
Dan Morgenstern-Kaplan ◽  
Ariel Cohen-Welch ◽  
Jair Lozano-Cuenca ◽  
Jorge López-Canales
Keyword(s):  
In Vivo Studies ◽  
Vasorelaxant Effect ◽  
Cardiovascular Side Effects ◽  
Clinical Benefits ◽  
Calcium Activated Potassium Channels ◽  
Vasodilating Activity ◽  
Treatment Of Obesity ◽  
Derivatives Of ◽  
Vasodilating Effect

Anorexigenics are compounds capable of reducing or suppressing appetite. Their three main types act on different neurotransmitters, either norepinephrine, serotonin or a combination of both. Among the drugs that act on norepinephrine are fenproporex, amfepramone and clobenzorex. Derivatives of the thyroid hormone triiodothyronine have also been associated with weight loss and used as a controversial treatment for obesity, despite their known cardiovascular side effects. Recent data suggest a possible vasodilating effect for these four substances that might be beneficial in a subset of patients. Herein we performed a systematic review of the literature (with emphasis on recent reports) to determine the implications and mechanisms of the vasodilating effects of some anorectics, specifically fenproporex, clobenzorex, amfepramone and triiodothyronine. Data analysis showed these four drugs to be vasodilating agents for rat aortic rings. The different mechanisms of action include endothelium-dependent vasodilation via activation of the NO-cGMP-PKG pathway and the opening of calcium-activated potassium channels. The finding of vasodilating activity indicates a potential role for some anorexigenic drugs in the treatment of obesity in hypertensive patients. Further in vivo studies are needed to test the clinical benefits of these four drugs.

scholarly journals STUDY OF THE AFFINITY OF N-ACYL DERIVATIVES OF 2-OXO-1-PYRROLIDINE ACETAMIDE TO THE BINDING SITE OF NMDA RECEPTOR BY MOLECULAR DOCKING METHOD

2019 ◽  
pp. 4-6
Author(s):  
A.S. Chiriapkin ◽  
A.A. Glushko ◽  
I.P. Kodonidi
Keyword(s):  
Biological Activity ◽  
Molecular Docking ◽  
Nmda Receptor ◽  
Binding Site ◽  
Computational Method ◽  
In Vivo Studies ◽  
Docking Method ◽  
Derivatives Of ◽  
Acyl Derivatives

The search for new compounds with а high nootropic biological activity is a promising scientific direction. A modern computational method for predicting pharmacological activity of the studied compounds is the molecular docking. The aim of this work is to study the affinity of new N-acyl derivatives of 2-oxo-1-pyrrolidine acetamide to the binding site of NMDA receptor to search of new effective nootropic drugs. As objects of study, there are used the new N-acyl derivatives of 2-oxo-1-pyrrolidine acetamide, racetams, glutamate and a virtual model of NMDA receptor of organism Rattus norvegicus with an identification code 2A5S from the RCSB PDB database. The results of the computational experiment indicate the presence of high nootropic biological activity in the compounds under study. Substance 3 has the greatest affinity of the N-acyl derivatives of 2-oxo-1-pyrrolidineethanol to the binding site of NMDA receptor Thus, we consider it is appropriate to conduct pharmacological in vivo studies of these compounds for the presence of nootropic biological activity.

scholarly journals Cysteine Derivatized 99mTc-Labelled Fatty Acids as β-Oxidation Markers

Inorganics ◽  
2019 ◽  
Vol 7 (11) ◽  
pp. 133
Author(s):  
Theodoros Tsotakos ◽  
Charalambos Triantis ◽  
Christos Kiritsis ◽  
Aggeliki Panagiotopoulou ◽  
Dimitrios Psimadas ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Myocardial Metabolism ◽  
Radiochemical Yield ◽  
In Vivo Studies ◽  
Rapid Clearance ◽  
Derivatives Of ◽  
Heart Uptake ◽  
Donor System

With the aim of developing 99mTc-labeled fatty acids intended for myocardial metabolism imaging we report herein the synthesis and characterization of two novel derivatives of undecanonoic and hexadecanonoic acid that have been functionalized at the ω-site by cysteine through the formation of a thioether bond (Cys–FA11 and Cys–FA16). Equimolar amounts of each ligand and the [NEt4]2[Re(CO)3Br3] precursor generated the respective hexacoordinated neutral complexes in which the ligand coordinated to the metal through the SNO donor system of cysteine. The rhenium complexes were characterized by elemental analysis, IR and NMR spectroscopies. The analogous technetium-99m complexes, 99mTc–Cys–FA11 and 99mTc–Cys–FA16 were prepared by incubation of the ligand with the precursor [99mTc(CO)3(H2O)3]+ (radiochemical yield ≥98%). Their structure was established by comparative HPLC techniques. In vivo studies in mice showed high initial heart uptake for both 99mTc complexes (7.4 ± 0.53 and 7.07 ± 0.73 percentage of injected dose (%ID)/g at 1 min post injection. Rapid clearance (0.60 ± 0.02 %ID/g) was observed for 99mTc–Cys–FA11 while the clearance of the longer fatty acid 99mTc–Cys–FA16 was slower (2.31 ± 0.09 %ID/g at 15 min p.i.). Metabolite analysis study indicated that complexes were catabolized through the β-oxidation process.

Synthesis, characterization and 99mTc-radiolabelling of specific derivatives of alpha thymosin peptides for in vitro and in vivo studies

2011 ◽  
Author(s):  
Chrysoula-Evangelia Karachaliou ◽  
Christos Zikos ◽  
Dimitra Benaki ◽  
Maria Pelecanou ◽  
Ourania Tsitsilonis ◽  
...  
Keyword(s):  
In Vivo Studies ◽  
Derivatives Of
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