School of Chemistry, University of Bristol, Cantock's Close, Bristol, BS8 1TS (UK).
Angew Chem Int Ed Engl. 2014 May 26;53(22):5609-13. doi: 10.1002/anie.201311071. Epub 2014 Apr 7.
Transmembrane anion carriers (anionophores) have potential for biological activity, including the treatment of channelopathies such as cystic fibrosis. A new family of anionophores has been synthesized, in which three thiourea groups are mounted on a cyclohexane-based scaffold. Though conceptually related to earlier polycyclic systems, these molecules are simpler and far more accessible. Preorganization is somewhat reduced compared to earlier systems, and anion affinities are correspondingly lower. However, transport activities set new records. This surprising performance suggests a role for controlled flexibility in the design of transmembrane anion carriers.
跨膜阴离子载体(阴离子载体)具有生物活性的潜力,包括治疗囊性纤维化等通道病。已经合成了一类新的阴离子载体,其中三个硫脲基团连接在环己烷骨架上。尽管这些分子在概念上与早期的多环系统有关,但它们更简单,也更容易获得。与早期的系统相比,预组织的程度有所降低,相应地阴离子亲和力也较低。然而,运输活性创下了新纪录。这种惊人的性能表明,在设计跨膜阴离子载体时,控制柔韧性起着重要作用。