YHU Scientific Journal, Vol 11, p73-84, 2024
STUDY OF THE ANTIOXIDANT PROPERTIES OF DIAMIDO DERIVATIVES OF SUCCINIC ACID IN THE BRAIN AND LIVER TISSUES OF WHITE RATS
H. Hunanyan, N. Pakhutyan, Sh. Stepanyan, G. Adzharyan, H.
Gasparyan, Q.Navoyan
Scientific and Technological Center of Organic Pharmaceutical Chemistry of the NAS RA,
YHU
Received 12.06.24, reviewed 07.07., accepted 17.07
DOI: 10.61484/29538181-sj.11.24-8
Abstract. Based on the high biological activity of diamide derivatives of succinic acid, diamide derivatives of succinic acid N1-((1-(3,4-dimethoxyphenyl)cyclopentyl) methyl)-N2-(4-bromophenyl))oxalamide with the conventional name 1.24.45, N1- ((1-(3,4-dimethoxyphenyl) cyclopentyl)methyl)-N2-(p-tolyl)oxalamide’ 1.24.46,N1- ((1-(3,4-dimethoxyphenyl) cyclopentyl) methyl)-N2-(3-(trifluoromethyl)phenyl) oxalamide’ -1,24,47 were synthesized at the Scientific and Technical Center of Physical Chemistry of the National Academy of Sciences of the Republic of Armenia by the method of intramolecular cyclization to study the antioxidant activity of these compounds. According to the results obtained, all three studied compounds exhibit antioxidant activity, and the absolute difference from the control is most pronounced for compound 1.24.47 (20.33% in the liver and 14.85% in the brain). Based on the theory of pharmacophore groups of imidazoline receptors, it can be concluded that the antioxidant activity of compounds 1.24.45, 1.24.46 and 1.24.47 may be due to their sensitivity to these receptors. Docking studies were then performed to identify and evaluate binding to these receptors. “Oxalic acid diamide derivatives” with the code names 1.24.45, 1.24.46 and 1.24.47 were found to bind to the active site of the target, exhibiting high similarity to the target molecule. Calculation of the drug-like properties of the compounds shows that they comply with the Lipinski rule in all aspects except the Log P value, and cannot penetrate the BBB. Thus, the results obtained provide a background for reco
Keywords: derivatives of succinic acid diamide, intramolecular cyclization method, antioxidant activity.mmending them as effective treatments for oxidative stress.
Abstract. Based on the high biological activity of diamide derivatives of succinic acid, diamide derivatives of succinic acid N1-((1-(3,4-dimethoxyphenyl)cyclopentyl) methyl)-N2-(4-bromophenyl))oxalamide with the conventional name 1.24.45, N1- ((1-(3,4-dimethoxyphenyl) cyclopentyl)methyl)-N2-(p-tolyl)oxalamide’ 1.24.46,N1- ((1-(3,4-dimethoxyphenyl) cyclopentyl) methyl)-N2-(3-(trifluoromethyl)phenyl) oxalamide’ -1,24,47 were synthesized at the Scientific and Technical Center of Physical Chemistry of the National Academy of Sciences of the Republic of Armenia by the method of intramolecular cyclization to study the antioxidant activity of these compounds. According to the results obtained, all three studied compounds exhibit antioxidant activity, and the absolute difference from the control is most pronounced for compound 1.24.47 (20.33% in the liver and 14.85% in the brain). Based on the theory of pharmacophore groups of imidazoline receptors, it can be concluded that the antioxidant activity of compounds 1.24.45, 1.24.46 and 1.24.47 may be due to their sensitivity to these receptors. Docking studies were then performed to identify and evaluate binding to these receptors. “Oxalic acid diamide derivatives” with the code names 1.24.45, 1.24.46 and 1.24.47 were found to bind to the active site of the target, exhibiting high similarity to the target molecule. Calculation of the drug-like properties of the compounds shows that they comply with the Lipinski rule in all aspects except the Log P value, and cannot penetrate the BBB. Thus, the results obtained provide a background for reco
Keywords: derivatives of succinic acid diamide, intramolecular cyclization method, antioxidant activity.mmending them as effective treatments for oxidative stress.