SAR study of 4-arylazo-3,5-diamino-1H-pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms,RSC Medicinal Chemistry

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SAR study of 4-arylazo-3,5-diamino-1H-pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-09-03 , DOI: 10.1039/d1md00275a
Charlotte U Jansen ₁ , Jesper Uhd ₁ , Jens B Andersen ₂ , Louise D Hultqvist ₂ , Tim H Jakobsen ₂ , Martin Nilsson ₂ , Thomas E Nielsen _{2,

3} , Michael Givskov ₂ , Tim Tolker-Nielsen ₂ , Katrine M Qvortrup ₁

Affiliation

By screening of a collection of 50 000 small-molecule compounds, we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of anti-biofilm agents. Here, we report a SAR study based on 60 analogues by examining ways in which the pharmacophore can be further optimized, for example, via substitutions in the aryl ring. The SAR study revealed the very potent anti-biofilm compound 4-(2-(2-fluorophenyl)hydrazineylidene)-5-imino-4,5-dihydro-1H-pyrazol-3-amine (2).

中文翻译：

4-arylazo-3,5-diamino-1H-pyrazoles 的 SAR 研究：鉴定诱导铜绿假单胞菌生物膜分散的小分子

通过筛选 50 000 种小分子化合物的集合，我们最近将 4-arylazo-3,5-diamino-1 H -pyrazoles 鉴定为一组新型抗生物膜剂。在这里，我们报告了一项基于 60 种类似物的 SAR 研究，通过检查可以进一步优化药效团的方法，例如通过芳环中的取代。SAR 研究揭示了非常有效的抗生物膜化合物 4-(2-(2-fluorophenyl)hydrazineylidene)-5-imino-4,5-dihydro-1 H -pyrazol-3-amine ( 2 )。

更新日期：2021-09-22

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