SYNTHESIS AND ANTIAGGREGANT ACTIVITY OF 2-CYCLOALKYLAMINO-5-THIENYL- AND -5-FURYL-6#-l,3,4-THIADIAZINES

O. N. Chupakhin; L. P. Sidorova; N. M. Perova; V. L. Rusinov; T. M. Vasileva; V. A. Makarov

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SYNTHESIS AND ANTIAGGREGANT ACTIVITY OF 2-CYCLOALKYLAMINO-5-THIENYL- AND -5-FURYL-6#-l,3,4-THIADIAZINES

机译：2-环烷基氨基-5-噻吩基和-5-FURYL-6＃-1,3,4-噻二嗪的合成及抗凝活性

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A series of new 5-(thienyl-2)-, 5-(furyl-2)-, and 5-(thienyl-3)-l,3,4-thiadiazme derivatives have been synthesized using methods based on the cyclocondensation of a-bromoacetylthiophenes or alpha-bromo-2-acetylfurans with 4-substitutedthiosemicarbazides. The effects of the synthesized compounds on human platelet aggregation in vitro and on rabbit platelet aggregation ex vivo have been studied. The most active 5-(thienyl-2)-1,3,4-thiadiazines inhibit human platelet aggregation induced by ADP and arachidonic acid in a broad concentration range. These compounds have good potential as emergency drugs for the treatment and prophylaxis of infarction and stroke.

机译：使用基于α-环缩合的方法合成了一系列新的5-（噻吩基-2）-，5-（呋喃基-2）-和5-（噻吩基-3）-1,3,4-噻二嗪衍生物。 -溴代乙酰基噻吩或α-溴代-2-乙酰基呋喃与4-取代的硫代氨基脲。研究了合成的化合物对体外人血小板聚集和离体兔血小板聚集的影响。最活跃的5-（噻吩基-2）-1,3,4-噻二嗪类化合物在很宽的浓度范围内均能抑制ADP和花生四烯酸诱导的人血小板聚集。这些化合物作为治疗和预防梗塞和中风的紧急药物具有良好的潜力。

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《Pharmaceutical Chemistry Journal》 |2011年第5期|共5页
作者
O. N. Chupakhin; L. P. Sidorova; N. M. Perova; V. L. Rusinov; T. M. Vasileva; V. A. Makarov;
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正文语种 eng
中图分类药学;
关键词
synthesis; 1; 3; 4-thiadiazines; platelet aggregation.;

机译：合成;1;3;4-噻二嗪;血小板聚集;

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1. SYNTHESIS AND ANTIAGGREGANT ACTIVITY OF 2-CYCLOALKYLAMINO-5-THIENYL- AND -5-FURYL-6#-l,3,4-THIADIAZINES [J] . O. N. Chupakhin, L. P. Sidorova, N. M. Perova, Pharmaceutical Chemistry Journal . 2011,第5期

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SYNTHESIS AND ANTIAGGREGANT ACTIVITY OF 2-CYCLOALKYLAMINO-5-THIENYL- AND -5-FURYL-6#-l,3,4-THIADIAZINES

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