Syntheses and in vitro evaluation of water-soluble "cationic metalloporphyrin-ellipticine" molecules having a high affinity for DNA

1991 ◽  
Vol 34 (3) ◽  
pp. 900-906 ◽  
Author(s):  
Li Ding ◽  
Guita Etemad-Moghadam ◽  
Suzy Cros ◽  
Christian Auclair ◽  
Bernard Meunier
Keyword(s):  
Water Soluble ◽  
In Vitro Evaluation ◽  
High Affinity

scholarly journals Synthesis and in vitro evaluation of new fluorinated quinoline derivatives with high affinity for PDE5: Towards the development of new PET neuroimaging probes

2017 ◽  
Vol 136 ◽  
pp. 548-560 ◽  
Author(s):  
Jianrong Liu ◽  
Aurélie Maisonial-Besset ◽  
Barbara Wenzel ◽  
Damien Canitrot ◽  
Ariane Baufond ◽  
...  
Keyword(s):  
Quinoline Derivatives ◽  
In Vitro Evaluation ◽  
High Affinity

Radiosynthesis and in vitro evaluation of 2-(N-alkyl-N-1′-11C-propyl)amino-5-hydroxytetralin analogs as high affinity agonists for dopamine D-2 receptors

1999 ◽  
Vol 26 (7) ◽  
pp. 725-735 ◽  
Author(s):  
Bingzhi Shi ◽  
Tanjore K Narayanan ◽  
Zhi-Ying Yang ◽  
Bradley T Christian ◽  
Jogeshwar Mukherjee
Keyword(s):  
In Vitro Evaluation ◽  
High Affinity ◽  
D 2 Receptors

Synthesis, in vitro and in silico studies of inhibitory activity towards α-amylase of bis-azole scaffolds linked by an alkylsulfanyl chain

2020 ◽  
Vol 98 (11) ◽  
pp. 725-735
Author(s):  
Vnira R. Akhmetova ◽  
Nail S. Akhmadiev ◽  
Radik A. Zainullin ◽  
Veronika R. Khayrullina ◽  
Ekaterina S. Mescheryakova ◽  
...  
Keyword(s):  
Active Site ◽  
Active Sites ◽  
Water Soluble ◽  
Human Pancreas ◽  
Diethyl Sulfide ◽  
High Affinity ◽  
Competitive Mechanism ◽  
In Silico Studies ◽  
Noncompetitive Inhibitor

Twelve new α,ω-bis[(3,5-dimethylpyrazol-4-yl)methylsulfanyl]alkanes linked by alkyl, diethyl sulfide, and triethyl dioxide spacers were prepared by the multicomponent reaction of acetylacetone, formaldehyde, α,ω-dithiols, and monosubstituted hydrazines. Testing of these products for inhibition of α-amylase enzyme in vitro showed that bis(N-methylpyrazolylmethylsulfanyl)ethane 4a inhibits the enzyme by the competitive mechanism. Meanwhile, the water-soluble adduct of bis(isoxazolylmethylsulfanyl)ethane 2 with HCl (2·HCl) is a noncompetitive inhibitor. The molecular docking results attest to high complementarity between the test molecules and the enzymes such as α-amylases from Aspergillus niger and human pancreas. Bis-pyrazole compounds 1, 1·HCl, and 4a and bis-isoxazole compounds 2 and 2·HCl positioned in the active site of both α-amylases form two closely spaced clusters. For all cases, the bioactive conformations of the modeled ligands were identified, demonstrating high affinity of the bis-azoles (1, 1·HCl, 2, 2·HCl, 4a) to the enzymes. Hydrogen bonds stabilizing their position in both α-amylases active sites were identified.

Synthesis and in vitro evaluation of 18F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET

2010 ◽  
Vol 20 (5) ◽  
pp. 1749-1751 ◽  
Author(s):  
Edward G. Robins ◽  
Yongjun Zhao ◽  
Imtiaz Khan ◽  
Anthony Wilson ◽  
Sajinder K. Luthra ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Nmda Receptor Antagonists ◽  
Receptor Antagonists ◽  
In Vitro Evaluation ◽  
High Affinity

scholarly journals In vitro evaluation of sustained released matrix tablets containing ibuprofen: a model poorly water-soluble drug

2016 ◽  
Vol 52 (4) ◽  
pp. 751-759 ◽  
Author(s):  
Wendy Leticia Guerra-Ponce ◽  
Sandra Leticia Gracia-Vásquez ◽  
Patricia González-Barranco ◽  
Ivonne Antonieta Camacho-Mora ◽  
Yolanda Araceli Gracia-Vásquez ◽  
...  
Keyword(s):  
Water Soluble ◽  
Matrix Tablets ◽  
In Vitro Evaluation ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug
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