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Research in Pharmaceutical Sciences، جلد ۱۷، شماره ۵، صفحات ۴۸۲-۴۹۲
عنوان فارسی
چکیده فارسی مقاله
کلیدواژه‌های فارسی مقاله
عنوان انگلیسی Design and synthesis of some novel triazine-tyrosine hybrids as potential agents for the treatment of multiple sclerosis
چکیده انگلیسی مقاله Background and purpose: One of the most noteworthy methods to slow down multiple sclerosis (MS) progress is a decrease of lymphocyte cells via S1P1 receptor modulating. Here, a series of S1P1 receptor modulators were designed and investigated for their ability to decrease lymphocytes in a rat model. Experimental approach: Molecular docking was performed to compare the binding mode of desired compounds 5a-f with fingolimod to the active site of the S1P1 receptor, theoretically. To prepare desired compounds, 5a-f, cyanuric chloride was reacted with different amines, a-f, which then converted to 4a-f compounds through reaction with N-boc-Tyr-OMe ester. Finally, deprotection of the carboxyl and amino groups was carried out to obtain 5a-f as final products. Lymphocyte counting in the rat model was carried out using flow cytometry to evaluate the efficacy of the suggested compounds. Findings / Results: All compounds exhibited lower binding energy than fingolimod. Compound 5e with ΔG = -8.10 kcal/mol was the best compound. The structure of the compounds was confirmed spectroscopically. The in vivo study proved that compounds 5b and 5a decreased the lymphocytes level at 0.3 and 3 mg/kg, respectively. Conclusion and implications: The desired compounds were well fitted in the receptor active site following molecular docking studies. The results of lymphocyte count revealed that compounds 5a and 5b with propyl and ethyl substitutes showed the maximum activity in vivo. Finally, the results of the present project can be used for forthcoming investigations towards the design and synthesis of novel potential agents for MS treatment.
کلیدواژه‌های انگلیسی مقاله Lymphocyte counts,Molecular docking,Multiple sclerosis,S1P1R modulator.
نویسندگان مقاله | Sajjad Saeidi
Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran. Isfahan Pharmaceutical Sciences Research Center, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Parvin Asadi
Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Farshid Hassanzadeh
Isfahan Pharmaceutical Sciences Research Center, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan, I.R. Iran. Department of Pharmacology and Toxicology, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Mehdi Aliomrani
Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran. Isfahan Pharmaceutical Sciences Research Center, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Ghadam Ali Khodarahmi


نشانی اینترنتی http://rps.mui.ac.ir/index.php/jrps/article/view/2144
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زبان مقاله منتشر شده en
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نوع مقاله منتشر شده Original Article
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