scholarly journals Synthesis and Pharmacological Activity of Urea and Thiourea Derivatives of 4-Azatricyclo[5.2.2.02,6]undec-8-ene-3,5-dione

2007 ◽  
Vol 55 (5) ◽  
pp. 796-799 ◽  
Author(s):  
Marta Struga ◽  
Jerzy Kossakowski ◽  
Ewa Kedzierska ◽  
Sylwia Fidecka ◽  
Joanna Stefan´ska
Keyword(s):  
Pharmacological Activity ◽  
Thiourea Derivatives ◽  
Derivatives Of

Synthesis and Pharmacological Activity of Urea and Thiourea Derivatives of 4-Azatricyclo[5.2.2.02,6]undec-8-ene-3,5-dione.

ChemInform ◽  
2007 ◽  
Vol 38 (45) ◽  
Author(s):  
Marta Struga ◽  
Jerzy Kossakowski ◽  
Ewa Kedzierska ◽  
Sylwia Fidecka ◽  
Joanna Stefanska
Keyword(s):  
Pharmacological Activity ◽  
Thiourea Derivatives ◽  
Derivatives Of

Synthesis and Pharmacological Activity of Thiourea Derivatives of 1,7,8,9-Tetramethyl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione

2009 ◽  
Vol 6 (6) ◽  
pp. 445-450 ◽  
Author(s):  
Marta Struga ◽  
Jerzy Kossakowski ◽  
Anna Koziol ◽  
Tateusz Lis ◽  
Ewa Kedzierska ◽  
...  
Keyword(s):  
Pharmacological Activity ◽  
Thiourea Derivatives ◽  
Derivatives Of

Synthesis and pharmacological activity of derivatives of quinoline and condensed quinolines

1978 ◽  
Vol 12 (7) ◽  
pp. 881-886 ◽  
Author(s):  
V. G. Granik ◽  
A. M. Zhidkova ◽  
S. S. Kiselev ◽  
R. G. Glushkov ◽  
A. I. Polezhaeva ◽  
...  
Keyword(s):  
Pharmacological Activity ◽  
Derivatives Of

Synthesis and pharmacological activity of some derivatives of 3, 5?-BI-1H-indole

1979 ◽  
Vol 13 (4) ◽  
pp. 385-389
Author(s):  
L. G. Chilikin ◽  
N. V. Gorelova ◽  
G. Ya. Shvarts ◽  
N. N. Suvorov
Keyword(s):  
Pharmacological Activity ◽  
Derivatives Of

„IN SILICO“ PREDICTION OF PHARMACOKINETIC PROPERTIES AND DRUGLIKENESS OF NOVEL THIOUREA DERIVATIVES OF NAPROXEN

2021 ◽  
Author(s):  
Nikola V. Nedeljković ◽  
◽  
Vladimir D. Dobričić ◽  
Marina Ž. Mijajlović ◽  
Gordana P. Radić ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Aromatic Amines ◽  
Gastrointestinal Absorption ◽  
Skin Permeability ◽  
Thiourea Derivatives ◽  
Barrier Permeability ◽  
Brain Barrier Permeability ◽  
Pharmacokinetic Properties ◽  
Inhibitory Potential ◽  
Derivatives Of

Masking the carboxyl group of naproxen with other functional groups may be a promising strategy to decrease its gastrointestinal toxicity. Thiourea moiety has been described as an important pharmacophore in a variety of pharmacologically active compounds, including anti-inflammatory, antiviral, anticancer, hypoglycemic and antimicrobial agents. Our research group has previously designed twenty novel thiourea derivatives of naproxen, containing amino acids (glycine, L-alanine, β-alanine, L-valine and L-phenylalanine – compounds 1,2,3,4 and 5, respectively), their methyl (6–10) and ethyl esters (11–15), as well as aromatic amines (16–20). Pharmacokinetic properties and druglikeness of these compounds were predicted using SwissADME web tool (http://www.swissadme.ch/). Predicted pharmacokinetic properties include potential for gastrointestinal absorption, blood-brain barrier permeability, skin permeability, transport mediated by P-glycoproteins and enzyme inhibitory potential. Druglikeness was evaluated using Lipinski’s, Ghose’s, Veber’s, Egan’s and Muegge’s rules, as well as on the basis of bioavailability score. All tested compounds had high-predicted gastrointestinal absorption and low blood-brain barrier permeability. Also, derivatives 2, 4, 7, 9, 10, 12, 14, 15 and 18 were predicted to be substrates for P-glycoprotein. Derivatives with aromatic amines (16–20) showed inhibitory potential against all tested CYP isoforms. Derivative 19 had the highest, while derivative 13 demonstrated the lowest predicted skin permeability. Finally, derivatives 1–12, except 5 and 10, have druglike structures, since they obey to all imposed rules.

Derivatives of the alkaloid convolvine and their pharmacological activity

2011 ◽  
Vol 47 (4) ◽  
pp. 608-611 ◽  
Author(s):  
A. M. Gapparov ◽  
I. I. Okhunov ◽  
S. F. Aripova ◽  
A. Nabiev ◽  
V. U. Khuzhaev
Keyword(s):  
Pharmacological Activity ◽  
Derivatives Of

Synthesis and pharmacological activity of derivatives of 1-(3-amino-2-hydroxypropyl)-5-methoxyindole

1988 ◽  
Vol 22 (8) ◽  
pp. 631-633
Author(s):  
E. K. Panisheva ◽  
T. K. Trubitsina ◽  
A. A. Cherkasova
Keyword(s):  
Pharmacological Activity ◽  
Derivatives Of

Synthesis, structural studies and biological activity of novel Cu(II) complexes with thiourea derivatives of 4-azatricyclo[5.2.1.0 2,6 ]dec-8-ene-3,5-dione

2017 ◽  
Vol 176 ◽  
pp. 8-16 ◽  
Author(s):  
Aleksandra Drzewiecka-Antonik ◽  
Paweł Rejmak ◽  
Marcin T. Klepka ◽  
Anna Wolska ◽  
Piotr Pietrzyk ◽  
...  
Keyword(s):  
Biological Activity ◽  
Structural Studies ◽  
Thiourea Derivatives ◽  
Derivatives Of
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