1,1,4-Derivatives of Thiosemicarbazide—New Non-Staining Antiozonants

1973 ◽  
Vol 46 (2) ◽  
pp. 517-523
Author(s):  
L. K. Zolotarevskaya ◽  
A. M. Lipkin ◽  
A. E. Grinberg ◽  
L. G. Angert
Keyword(s):  
Protective Effect ◽  
Rate Constant ◽  
Practical Interest ◽  
Initial Reaction ◽  
Inhibiting Activity ◽  
Thiourea Derivatives ◽  
New Class ◽  
Mechanism Of Reaction ◽  
Thiosemicarbazide Derivatives ◽  
Derivatives Of

Abstract In the nature of non-staining antiozonants, a new class of compounds, 1,1,4-derivatives of thiosemicarbazide, are proposed. The mechanism of reaction of thiosemicarbazide derivatives with ozone is analogous to the mechanism of this reaction with thiourea derivatives. Within this, the rate constant of the initial reaction of the thiosemicarbazide derivatives with ozone is somewhat higher than that of the thiourea derivatives. 1,1,4-Trialkyl-substituted thiosemicarbazides appear to be the most effective antiozonants, not changing the color of light vulcanizates. Of the investigated compounds, 1,1,4-tributylthiosemicarbazide, being distinguished by a large protective effect against ozone, inhibiting activity in the process of heat aging of the vulcanizates, and lesser ability for leaching out of the vulcanizates by water than tributylthiourea, presents the greatest practical interest.

Some 6-substituted derivatives of D-8-cyanomethylergoline-I and D-8-methylergoline-I

1979 ◽  
Vol 44 (3) ◽  
pp. 946-951 ◽  
Author(s):  
Antonín Černý ◽  
Jiří Křepelka ◽  
Miroslav Semonský
Keyword(s):  
Inhibiting Activity ◽  
Chloro Derivatives ◽  
Derivatives Of

Compounds III-XX exhibiting antilactation and antinidation effects in tests on rats were prepared on N(6)-alkylation of D-8-cyanomethylergoline-I (I) or D-8-methylergoline-I (II) with corresponding bromo (chloro) derivatives in dimethylformamide. The most distinct prolactin-inhibiting activity was found in compound III.

„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.

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 Reactions of Some New Quinoline Thiosemicarbazide Derivatives of Potential Biological Activity

2008 ◽  
Vol 183 (6) ◽  
pp. 1323-1343 ◽  
Author(s):  
E. M. Keshk ◽  
S. I. El-Desoky ◽  
M. A. A. Hammouda ◽  
A. H. Abdel-Rahman ◽  
A. G. Hegazi
Keyword(s):  
Biological Activity ◽  
Potential Biological Activity ◽  
Thiosemicarbazide Derivatives ◽  
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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