Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study.,RSC Medicinal Chemistry

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Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study.
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2019-08-15 , DOI: 10.1039/c9md00286c
Pasquale Linciano ₁ , Barbara De Filippis ₂ , Alessandra Ammazzalorso ₂ , Pasquale Amoia ₂ , Felisa Cilurzo ₂ , Marialuigia Fantacuzzi ₂ , Letizia Giampietro ₂ , Cristina Maccallini ₂ , Charlotte Petit ₃ , Rosa Amoroso ₂

Affiliation

PPAR agonists represent a new therapeutic opportunity for the prevention and treatment of neurodegenerative disorders, but their pharmacological success depends on favourable pharmacokinetic properties and capability to cross the BBB. In this study, we assayed some PPAR agonists previously synthesized by us for their physicochemical properties, with particular references to lipophilicity, solubility and permeability profiles, using the PAMPA. Although tested compounds showed high lipophilicity and low aqueous solubility, the results revealed a good overall druggability profile, encouraging further studies in the field of neurodegenerative diseases.

中文翻译：

二苯乙烯衍生的 PPAR 激动剂的成药性概况：理化性质的测定和 PAMPA 研究。

PPAR 激动剂代表了预防和治疗神经退行性疾病的新治疗机会，但其药理学成功取决于良好的药代动力学特性和穿过血脑屏障的能力。在这项研究中，我们使用 PAMPA 分析了我们之前合成的一些 PPAR 激动剂的理化性质，特别是亲脂性、溶解度和渗透性特征。尽管测试的化合物表现出高亲脂性和低水溶性，但结果显示出良好的整体成药性，鼓励神经退行性疾病领域的进一步研究。

更新日期：2019-08-15

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