Derivative containing 4-piperazinyl anilino and 2-piperazinyl propionamido and application of derivative in preparation of anti-pulmonary fibrosis medicine

The invention belongs to the field of medicines, and discloses a novel derivative containing 4-piperazinyl aniline and 2-piperazinyl propionamido, and the structural formula of the derivative is shown as any one of a formula I or a formula II. Cellular level and in vivo tests prove that the derivati...

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Bibliographische Detailangaben
Hauptverfasser: REN YUANYUAN, GU CHENXI, ZHAO WENJING, HU WENHAO, YAO HAN, ALBERT SUNI CHAN, LI XINGSHU
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the field of medicines, and discloses a novel derivative containing 4-piperazinyl aniline and 2-piperazinyl propionamido, and the structural formula of the derivative is shown as any one of a formula I or a formula II. Cellular level and in vivo tests prove that the derivative containing the 4-piperazinyl aniline group and the 2-piperazinyl propionamido group is good in pulmonary fibrosis resisting activity and high in bioavailability, and has better activity and pharmacokinetic properties compared with an existing positive drug nintedanib. Meanwhile, the series of derivatives are simple in synthesis process and low in cost, and have good application prospects. # imgabs0 # 本发明属于药物领域,公开了新型含4-哌嗪基苯胺基及2-哌嗪基丙酰胺基衍生物,所述衍生物的结构式为式I或II任一所示。本发明中含4-哌嗪基苯胺基及2-哌嗪基丙酰胺基衍生物在细胞水平和体内试验中验证了其抗肺纤维化活性好,且生物利用度高,具有较现有的阳性药物尼达尼布更优的活性和药代动力学性质。同时,该系列衍生物合成工艺简单,成本低廉,具有较好的应用前景。#imgabs0#