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Physicochemical Properties of Zwitterionic Drugs in Therapy.
ChemMedChem ( IF 3.4 ) Pub Date : 2020-05-20 , DOI: 10.1002/cmdc.202000164
Károly Mazák 1 , Béla Noszál 1
Affiliation  

In solution, amphoteric compounds exist in anionic, uncharged, zwitterionic and cationic forms. The importance of zwitterionic drugs is currently under‐represented in the literature. Herein, the acid‐base parameters, lipophilicity and solubility of such compounds are discussed to deepen the molecular‐level understanding of their pharmacokinetic and pharmacodynamic behaviour. Our recent studies show there are many drug molecules, including thyroid hormones and 5‐hydroxytryptophan, the precursor of the neurotransmitter serotonin, for which the contribution of the zwitterionic microspecies to the overall lipophilicity exceeds that of the uncharged one, which is of higher individual lipophilicity, but occurs in much lower concentration. The second part of the minireview highlights the most important zwitterionic compounds in therapy, grouped into therapeutic classes. The importance of the charge of the molecules is emphasized in their binding to the target molecules.

中文翻译:

两性离子药物在治疗中的理化特性。

在溶液中,两性化合物以阴离子,不带电,两性离子和阳离子形式存在。两性离子药物的重要性目前在文献中并未得到充分体现。在此,我们讨论了这类化合物的酸碱参数,亲脂性和溶解性,以加深对药物动力学和药效学行为的分子水平的了解。我们最近的研究表明,有许多药物分子,包括甲状腺激素和5-羟色氨酸(神经递质5-羟色胺的前体),两性离子微生物对总体亲脂性的贡献超过了不带电荷的物种,后者的亲脂性更高。 ,但浓度要低得多。minireview的第二部分重点介绍了治疗中最重要的两性离子化合物,分为治疗类别。在分子与靶分子的结合中强调了分子电荷的重要性。
更新日期:2020-07-03
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