Synthesis and Pharmacological Activity of S(-)-2-Amino-2-Methyl-3-Phenylpropanoic Acid
- Авторы: Grigoryan S.1, Zhamharyan A.1, Saghyan A.2, Chitchiyan A.1, Balyan L.1, Poghosyan A.2, Topchyan H.1, Balasanyan M.1
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Учреждения:
- M. Heratsi Yerevan State Medical University
- Research and Production Center “Armbiotechnology”, National Academy of Sciences of Armenia
- Выпуск: Том 53, № 7 (2019)
- Страницы: 620-623
- Раздел: Article
- URL: https://journals.rcsi.science/0091-150X/article/view/245902
- DOI: https://doi.org/10.1007/s11094-019-02049-1
- ID: 245902
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Аннотация
Taking into account the high efficacy of 2-arylpropionic acid derivatives among NSAIDs and based on their SARs, we have evaluated the anti-inflammatory, antinociceptive, and antiaggregant activity and ulcerogenic properties of a new synthesized non-protein amino acid (NPAA) derivative S(-)-2-amino-2-methyl-3-phenylpropanoic acid (NPAA-36). A new method of NPAA-36 synthesis was developed and experiments were carried out, which showed that this compound injected in a dose of 10 mg/kg (i.p.) inhibited xylene-induced ear oedema by about 31.1%, which proved its anti-inflammatory properties. The antinociceptive activity of NPAA-36 was assessed in tail-flick test by the ability to increase the tail cut-off latency by 36.78% within 60 min after injection at the same dose. Investigation of the ulcerogenic properties of NPAA-36 demonstrated that it exhibited lower gastrointestinal toxicity than a well-known arylpropionic acid derivative NSAID. Results of in vitro experiments showed the antiplatelet activity registered not in all (only in 41.2%) cases, which might imply lower bleeding. The obtained data indicate that the new NPAAderivative can be a potential basis for the development of new anti-inflammatory drugs with weak side effects.
Об авторах
S. Grigoryan
M. Heratsi Yerevan State Medical University
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0025
A. Zhamharyan
M. Heratsi Yerevan State Medical University
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0025
A. Saghyan
Research and Production Center “Armbiotechnology”, National Academy of Sciences of Armenia
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0056
A. Chitchiyan
M. Heratsi Yerevan State Medical University
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0025
L. Balyan
M. Heratsi Yerevan State Medical University
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0025
A. Poghosyan
Research and Production Center “Armbiotechnology”, National Academy of Sciences of Armenia
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0056
H. Topchyan
M. Heratsi Yerevan State Medical University
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0025
M. Balasanyan
M. Heratsi Yerevan State Medical University
Автор, ответственный за переписку.
Email: mara.balasanyan@gmail.com
Армения, Yerevan, 0025