Design and synthesis of specific colivelin derivatives for in vitro and in vivo studies

2011 ◽  
Author(s):  
Myrta Kostomoiri ◽  
Christos Zikos ◽  
Dimitra Benaki ◽  
Jiřina Slaninová ◽  
Ioannis Pirmettis ◽  
...  
Keyword(s):  
In Vivo Studies ◽  
Design And Synthesis

The design and synthesis of novel orally active inhibitors of AP-1 and NF-κB mediated transcriptional activation. SAR of In vitro and In vivo studies

2003 ◽  
Vol 13 (22) ◽  
pp. 4077-4080 ◽  
Author(s):  
Moorthy S.S. Palanki ◽  
Paul E. Erdman ◽  
Minghuan Ren ◽  
Mark Suto ◽  
Brydon L. Bennett ◽  
...  
Keyword(s):  
Transcriptional Activation ◽  
In Vivo Studies ◽  
Design And Synthesis ◽  
Orally Active

Nanocarriers for Vaccine and Gene Delivery Application

2018 ◽  
pp. 381-414 ◽  
Author(s):  
Behiye Şenel ◽  
Gülay Büyükköroğlu
Keyword(s):  
Genetic Material ◽  
Biological Properties ◽  
Target Site ◽  
Inorganic Nanoparticles ◽  
In Vivo Studies ◽  
Polymeric Systems ◽  
Design And Synthesis ◽  
Vaccine Antigens

Nanocarriers with various compositions and biological properties are frequently used systems for in-vitro/in-vivo vaccination and gene transfer. In recent years, developments in nanotechnology have focused on the design and synthesis of nanocarriers that have new properties and can be modified for gene and vaccine delivery. In the favorable results obtained from in-vivo studies performed, they increase interest in these developments and pave the way for their therapeutic use. Nanocarriers have become increasingly important because they can stabilize vaccine antigens and serve as adjuvants, with the advantage of easily transporting genetic material to the target site. In nanocarriers, the molecules involved are adsorbed to the surface or encapsulated in particulates. At the same time, surface modification of nanoparticles allows these systems to carry cargo molecules easily to target site. Among the most studied nanocarriers, lipidic and polymeric systems dendrimers, inorganic nanoparticles, cyclodextrins, cell penetration peptides, and ISCOMs are attracting attention.

scholarly journals Design and Synthesis of Novel Thiazolo[5,4-d]Pyrimidine Derivatives with High Affinity for Both the Adenosine A1 and A2A Receptors, and Efficacy in Animal Models of Depression

2021 ◽  
Vol 14 (7) ◽  
pp. 657
Author(s):  
Flavia Varano ◽  
Daniela Catarzi ◽  
Erica Vigiani ◽  
Diego Dal Ben ◽  
Michela Buccioni ◽  
...  
Keyword(s):  
Preference Test ◽  
Tail Suspension Test ◽  
Docking Studies ◽  
In Vivo Studies ◽  
A2a Receptors ◽  
Design And Synthesis ◽  
Sucrose Preference Test ◽  
New Compounds

New compounds with a 7-amino-2-arylmethyl-thiazolo[5,4-d]pyrimidine structure were synthesized and evaluated in vitro for their affinity and/or potency at the human (h) A1, hA2A, hA2B, and hA3 adenosine receptors (ARs). Several compounds (5, 8–10, 13, 18–19) were characterized by nanomolar and subnanomolar binding affinities for the hA1 and the hA2A AR, respectively. Results of molecular docking studies supported the in vitro results. The 2-(2-fluorobenzyl)-5-(furan-2yl)-thiazolo[5,4-d]pyrimidin-7-amine derivative 18 (hA1 Ki = 1.9 nM; hA2A Ki = 0.06 nM) was evaluated for its antidepressant-like activity in in vivo studies, the forced swimming test (FST), the tail suspension test (TST), and the sucrose preference test (SPT) in mice, showing an effect comparable to that of the reference amitriptyline.

scholarly journals Design, Synthesis, and Validation of a Novel [11C]Promethazine PET Probe for Imaging Abeta Using Autoradiography

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2182
Author(s):  
Clayton A. Whitmore ◽  
Mariam I. Boules ◽  
William J. Behof ◽  
Justin R. Haynes ◽  
Dmitry Koktysh ◽  
...  
Keyword(s):  
Radiochemical Purity ◽  
In Vivo Studies ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
Molar Activity ◽  
Rp Hplc ◽  
Model Of Alzheimer’S Disease ◽  
Antihistamine Drug

Promethazine, an antihistamine drug used in the clinical treatment of nausea, has been demonstrated the ability to bind Abeta in a transgenic mouse model of Alzheimer’s disease. However, so far, all of the studies were performed in vitro using extracted tissues. In this work, we report the design and synthesis of a novel [11C]promethazine PET radioligand for future in vivo studies. The [11C]promethazine was isolated by RP-HPLC with radiochemical purity >95% and molar activity of 48 TBq/mmol. The specificity of the probe was demonstrated using human hippocampal tissues via autoradiography.

Design and Synthesis of a Biocompatible 1D Coordination Polymer as Anti-Breast Cancer Drug Carrier, 5-Fu: In Vitro and in Vivo Studies

2018 ◽  
Vol 10 (21) ◽  
pp. 17594-17604 ◽  
Author(s):  
Mahsa Rezaei ◽  
Alireza Abbasi ◽  
Rassoul Dinarvand ◽  
Mahmood Jeddi-Tehrani ◽  
Jan Janczak
Keyword(s):  
Breast Cancer ◽  
Coordination Polymer ◽  
Drug Carrier ◽  
In Vivo Studies ◽  
Cancer Drug ◽  
Design And Synthesis ◽  
1D Coordination Polymer

Design and synthesis of new carbamates as inhibitors for fatty acid amide hydrolase and cholinesterases: Molecular dynamic, in vitro and in vivo studies

2021 ◽  
Vol 109 ◽  
pp. 104684
Author(s):  
Mahdi Faal Maleki ◽  
Hamid Nadri ◽  
Mostafa Kianfar ◽  
Najmeh Edraki ◽  
Farhad Eisvand ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Molecular Dynamic ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
In Vivo Studies ◽  
Design And Synthesis ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

scholarly journals Phenylethynylbenzyl-modified biguanides inhibit pancreatic cancer tumor growth

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Audrey Hébert ◽  
Maxime Parisotto ◽  
Marie-Camille Rowell ◽  
Alexandra Doré ◽  
Ana Fernandez Ruiz ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Clinical Trials ◽  
Living Cells ◽  
In Vivo Studies ◽  
Design And Synthesis ◽  
Pancreatic Cancer Cells ◽  
Nadh Ratio ◽  
Cancer Tumor

AbstractWe present the design and synthesis of a small library of substituted biguanidium salts and their capacity to inhibit the growth of pancreatic cancer cells. We first present their in vitro and membrane activity, before we address their mechanism of action in living cells and in vivo activity. We show that phenylethynyl biguanidium salts possess higher ability to cross hydrophobic barriers, improve mitochondrial accumulation and anticancer activity. Mechanistically, the most active compound, 1b, like metformin, activated AMPK, decreased the NAD+/NADH ratio and mitochondrial respiration, but at 800-fold lower concentration. In vivo studies show that compound 1b significantly inhibits the growth of pancreatic cancer xenografts in mice, while biguanides currently in clinical trials had little activity.

scholarly journals Strong Inhibitory Activity and Action Modes of Synthetic Maslinic Acid Derivative on Highly Pathogenic Coronaviruses: COVID-19 Drug Candidate

Pathogens ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 623
Author(s):  
Raya Soltane ◽  
Amani Chrouda ◽  
Ahmed Mostafa ◽  
Ahmed A. Al-Karmalawy ◽  
Karim Chouaïb ◽  
...  
Keyword(s):  
Docking Study ◽  
In Vivo Studies ◽  
Drug Candidate ◽  
Molecular Docking Study ◽  
Maslinic Acid ◽  
Human Interface ◽  
Design And Synthesis ◽  
Novel Coronavirus

In late December 2019, a novel coronavirus, namely severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), escaped the animal–human interface and emerged as an ongoing global pandemic with severe flu-like illness, commonly known as coronavirus disease 2019 (COVID-19). In this study, a molecular docking study was carried out for seventeen (17) structural analogues prepared from natural maslinic and oleanolic acids, screened against SARS-CoV-2 main protease. Furthermore, we experimentally validated the virtual data by measuring the half-maximal cytotoxic and inhibitory concentrations of each compound. Interestingly, the chlorinated isoxazole linked maslinic acid (compound 17) showed promising antiviral activity at micromolar non-toxic concentrations. Thoughtfully, we showed that compound 17 mainly impairs the viral replication of SARS-CoV-2. Furthermore, a very promising SAR study for the examined compounds was concluded, which could be used by medicinal chemists in the near future for the design and synthesis of potential anti-SARS-CoV-2 candidates. Our results could be very promising for performing further additional in vitro and in vivo studies on the tested compound (17) before further licensing for COVID-19 treatment.

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