SCREENING OF WOUND-HEALING ACTIVITY OF N1-HYDRAZONOPROPYL DERIVATIVES OF TIETHANE-CONTAINING 6-METHYLURACIL
Abstract
Recently, pyrimidine derivatives are increasingly being used in medicine and pharmacology, showing high activity in the treatment of various diseases: Alzheimer's disease, viral infections, mycotic and microbial lesions, malignant tumors, wound healing pathologies of various etiologies.
Aim. Synthesis of new thietane-containing hydrazonopropyl derivatives of pyrimidine bases and analysis of their wound healing activity.
Material and methods. New hydrazone derivatives were obtained by reacting thietan, oxo- and dioxothietane-containing 6- methylpyrimidine-2,4(1H,3H)-dione with 1-chloropropan-2-one, followed by condensation with isonicotinic acid hydrazide. The structure and identity of the synthesized compounds were confirmed by nuclear magnetic resonance and infrared spectra, thin layer chromatography, elemental analysis and melting point determination. Preliminary prediction of acute toxicity was carried out in silico using the pkCSM web service and in vivo according to the standard method (Litchfield J. and Wilcoxon F.) modified by V.B. Prozorovsky.
Results. A preliminary prediction of the wound-healing activity of new hydrazonopropyl derivatives of 6-methylpyrimidine2,4(1H,3H)-dione was carried out using the integrated online platform Way2Drag.
Determination of the wound healing effect of the most active hydrazone derivative was carried out in vivo under a linear wound model on laboratory mice.
Preliminary screening of the wound-healing activity of the synthesized hydrazone derivatives made it possible to identify new active stimulators of wound-healing processes and identify some qualitative and quantitative structure-activity patterns, also with the help of the ADMET Prediction Service.
Conclusions. As a result of the study, new N1-hydrazone derivatives of thietane-containing 6-methyluracil were obtained, new biologically active molecules were identified that exhibited the effect of stimulating wound healing.
About the Authors
A. S. Melnikov
ФГБОУ ВО «Башкирский государственный медицинский университет» Минздрава России
Russian Federation
Russian Federation
S. A. Meshcheryakova
ФГБОУ ВО «Башкирский государственный медицинский университет» Минздрава России
Russian Federation
Russian Federation
A. V. Samorodov
ФГБОУ ВО «Башкирский государственный медицинский университет» Минздрава России
Russian Federation
Russian Federation
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Review
For citations:
Melnikov A.S., Meshcheryakova S.A., Samorodov A.V. SCREENING OF WOUND-HEALING ACTIVITY OF N1-HYDRAZONOPROPYL DERIVATIVES OF TIETHANE-CONTAINING 6-METHYLURACIL. Bashkortostan Medical Journal. 2024;19(3):43-47. (In Russ.)
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