The inhibition of δ- and η-class carbonic anhydrases (CAs; EC 4.2.1.1) was poorly investigated so far. Only one δ-CA, TweCA from the diatom Thalassiosira weissflogii, and one η-CA, PfCA, from Plasmodium falciparum, have been cloned and characterised to date. To enrich δ- and η-CAs inhibition profiles, a panel of 22 phenols was investigated for TweCA and PfCA inhibition. Some derivatives showed effective, sub-micromolar inhibition of TweCA (KIs 0.81-65.4 µM) and PfCA (KIs 0.62-78.7 µM). A subset of compounds demonstrated a significant selectivity for the target CAs over the human physiologically relevant ones. This study promotes the identification of new potent and selective inhibitors of TweCA and PfCA, which could be considered as leads for finding molecular probes in the study of carbon fixation processes (in which TweCA and orthologue enzymes are involved) or drug candidates in the treatment of malaria.

中文翻译：

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用酚类化合物对海洋硅藻thalassiosira weissflogii和原生动物恶性疟原虫的δ-和η-类碳酸酐酶的抑制作用调查。

到目前为止，对δ和η类碳酸酐酶（CAs; EC 4.2.1.1）的抑制作用研究很少。迄今为止，仅克隆和表征了来自硅藻Thalassiosira weissflogii的一个δ-CATweCA和来自恶性疟原虫的一个η-CAPfCA。为了丰富δ-和η-CAs抑制谱，研究了22种苯酚对TweCA和PfCA的抑制作用。一些衍生物对TweCA（KIs 0.81-65.4 µM）和PfCA（KIs 0.62-78.7 µM）表现出有效的亚微摩尔抑制作用。化合物的一个子集显示出对目标CA的选择性高于人类生理相关的CA。这项研究促进了TweCA和PfCA的新的有效和选择性抑制剂的鉴定，