Suppr超能文献

2-(2,4-二氟苯基)-1-[(1H-吲哚-3-基甲基)甲氨基]-3-(1H-1,2,4-三唑-1-基)丙-2-醇的合成及体外抗真菌活性评价。

Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1-[(1H-indol-3-ylmethyl)methylamino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols.

机构信息

Université de Nantes, Nantes Atlantique Universités, Département de Pharmacochimie, Cibles et Médicaments des Infections, de l'Immunité et du Cancer, IICIMED-EA 1155, UFR Sciences Pharmaceutiques, Nantes, France.

出版信息

J Enzyme Inhib Med Chem. 2011 Apr;26(2):261-9. doi: 10.3109/14756366.2010.503607. Epub 2010 Aug 9.

Abstract

We extended our previous studies based on the design of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents toward the identification of new indol-3-ylmethylamino derivatives. The majority of these compounds exhibited antifungal activity against a Candida albicans strain (minimum inhibitory concentrations ranging from 199.0 to 381.0 ng/mL) suggesting an inhibition of 14α-demethylase by sterol analysis studies, but are weaker inhibitors compared to their indol-5-ylmethylamino analogs.

摘要

我们基于 1-[(1H-吲哚-5-基甲基)氨基]-2-苯基-3-(1H-1,2,4-三唑-1-基)丙-2-醇类抗真菌药物的设计,进行了进一步的研究,以鉴定新的吲哚-3-基甲基氨基衍生物。这些化合物中的大多数对白色念珠菌菌株表现出抗真菌活性(最低抑制浓度范围为 199.0 至 381.0ng/mL),这表明甾醇分析研究中 14α-脱甲基酶受到抑制,但与它们的吲哚-5-基甲基氨基类似物相比,它们的抑制作用较弱。

相似文献

1
Synthesis and in vitro antifungal evaluation of 2-(2,4-difluorophenyl)-1-[(1H-indol-3-ylmethyl)methylamino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols.
J Enzyme Inhib Med Chem. 2011 Apr;26(2):261-9. doi: 10.3109/14756366.2010.503607. Epub 2010 Aug 9.
4
Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols.
Bioorg Med Chem Lett. 2009 Oct 15;19(20):5833-6. doi: 10.1016/j.bmcl.2009.08.089. Epub 2009 Aug 31.
5
Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents.
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1820-4. doi: 10.1016/j.bmcl.2008.02.027. Epub 2008 Feb 14.
7
Design, synthesis, and antifungal activity of novel conformationally restricted triazole derivatives.
Arch Pharm (Weinheim). 2009 Dec;342(12):732-9. doi: 10.1002/ardp.200900103.
8
Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
Bioorg Med Chem Lett. 2008 Jun 1;18(11):3261-5. doi: 10.1016/j.bmcl.2008.04.056. Epub 2008 Apr 25.
9
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4471-5. doi: 10.1016/j.bmcl.2011.06.008. Epub 2011 Jun 15.

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验