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查尔酮-噻唑衍生物对人体淋巴丝虫寄生虫马来布鲁线虫的合成及抗丝虫活性

Synthesis and antifilarial activity of chalcone-thiazole derivatives against a human lymphatic filarial parasite, Brugia malayi.

作者信息

Sashidhara Koneni V, Rao K Bhaskara, Kushwaha Vikas, Modukuri Ram K, Verma Richa, Murthy P K

机构信息

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, Uttar Pradesh 226031, India.

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, Uttar Pradesh 226031, India.

出版信息

Eur J Med Chem. 2014 Jun 23;81:473-80. doi: 10.1016/j.ejmech.2014.05.029. Epub 2014 May 12.

Abstract

Here we report the synthesis of novel chalcone-thiazole compounds and their antifilarial activity. The antifilarial properties of these hybrids were assessed against microfilariae as well as adult worms of Brugia malayi. Among all the synthesized compounds, only two compounds, namely 4g and 4n were identified to be promising in vitro. These active compounds were tested in B. malayi-jird (Meriones unguiculatus) and B. malayi-Mastomys coucha models. Compound 4n showed 100% embryostatic effect and 49% macrofilaricidal in jirds and M. coucha models, respectively. This study provides a new structural clue for the development of novel antifilarial lead molecules.

摘要

在此,我们报告新型查尔酮 - 噻唑化合物的合成及其抗丝虫活性。评估了这些杂化物对马来布鲁线虫微丝蚴以及成虫的抗丝虫特性。在所有合成化合物中,仅4g和4n这两种化合物在体外被鉴定为有前景。在马来布鲁线虫 - 沙鼠(长爪沙鼠)和马来布鲁线虫 - 冈比亚多乳鼠模型中对这些活性化合物进行了测试。化合物4n在沙鼠和冈比亚多乳鼠模型中分别显示出100%的胚胎抑制作用和49%的杀成虫作用。本研究为新型抗丝虫先导分子的开发提供了新的结构线索。

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