Abstract

Topicality. This article presents the results of the study of the biological activity of newly synthesized 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines. The acute toxicity of 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines was determined experimentally on non-linear white male mice with a total weight of 1620 g. A generation model was used to experimentally evaluate the analgesic activity acetic writhing in male mice. It was experimentally confirmed that the new synthesized 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines were non-toxic and had pronounced analgesic activity.
 Aim: to study the biological activity of the new synthesized 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines.
 Materials and methods. The prediction of the likely types of biological activity was carried out with the use of PASS computer program. The acute toxicity of 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines was determined experimentally on non-linear white male mice. Analgesic activity was established on a model of acetic acid writhing in mice.
 Results. 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines were classified as non-toxic substances (LD50 2000 mg / kg). The analgesic activity of the test compounds was higher than that of the reference drug.
 Conclusion. The new synthesized 6-[(1-naphthylmethyl]thio)-4-chloropyrazolo[3,4-d]pyrimidines are non-toxic and have pronounced analgesic activity.

Highlights

  • Федеральное государственное бюджетное образовательное учреждение высшего образования «Санкт‐Петербургский государственный химико-фармацевтический университет» Министерства здравоохранения Российской Федерации, Санкт-Петербург

  • This article presents the results of the study of the biological activity of newly synthesized 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines

  • Analgesic activity was established on a model of acetic acid “writhing” in mice

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Summary

Аспирантский вестник Поволжья

147 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines was determined experimentally on non-linear white male mice. Analgesic activity was established on a model of acetic acid “writhing” in mice. 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines were classified as non-toxic substances (LD50 — 2000 mg / kg). The new synthesized 6-[(1-naphthylmethyl]thio)-4-chloropyrazolo[3,4-d]pyrimidines are non-toxic and have pronounced analgesic activity. ■■ Keywords: 6-[(1-naphthylmethyl)thio]-4-chloropyrazolo[3,4-d]pyrimidines; biological activity; PASS program; acute toxicity; analgesic activity. Среди пиразолопиримидинов были выявлены вещества, проявляющие проти­вовирусную [9, 6], противомикробную [3, 12], противовоспалительную [10] активности. В последние несколько десятилетий интерес к этим соединения продолжает расти благодаря открытию их противоопухолевой активности [7, 11]. В связи с чем авторы приняли решение о поиске новых пиразоло[3,4‐d]­пири­мидинов и изучении их биологической активности. Цель работы — изучение биологической активности новых синтезированных 6-[(1-нафтилметил)тио]-4-хлорпиразоло[3,4-d]пиримидинов

Методы и материалы
Aspirantskiy Vestnik Povolzhiya
Результаты предварительного скрининга
Метамизол натрия
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