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Comparative chemical and biological hydrolytic stability of homologous esters and isosteres

التفاصيل البيبلوغرافية
العنوان: Comparative chemical and biological hydrolytic stability of homologous esters and isosteres
المؤلفون: Hygor M. R. de Souza, Jéssica S. Guedes, Rosana H. C. N. Freitas, Luis G. V. Gelves, Harold H. Fokoue, Carlos Mauricio R. Sant’Anna, Eliezer J. Barreiro, Lidia M. Lima
المصدر: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 718-727 (2022)
بيانات النشر: Taylor & Francis Group, 2022.
سنة النشر: 2022
المجموعة: LCC:Therapeutics. Pharmacology
مصطلحات موضوعية: esters, plasma and microsomal stability, homologous and isosteres, Therapeutics. Pharmacology, RM1-950
الوصف: Esters are one of the major functional groups present in the structures of prodrugs and bioactive compounds. Their presence is often associated with hydrolytic lability. In this paper, we describe a comparative chemical and biological stability of homologous esters and isosteres in base media as well as in rat plasma and rat liver microsomes. Our results provided evidence for the hydrolytic structure lability relationship and demonstrated that the hydrolytic stability in plasma and liver microsome might depend on carboxylesterase activity. Molecular modelling studies were performed in order to understand the experimental data. Taken together, the data could be useful to design bioactive compounds or prodrugs based on the correct choice of the ester subunit, addressing compounds with higher or lower metabolic lability.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1475-6366
1475-6374
14756366
Relation: https://doaj.org/toc/1475-6366; https://doaj.org/toc/1475-6374
DOI: 10.1080/14756366.2022.2027933
URL الوصول: https://doaj.org/article/fbb8bd8c8d3b4bd2995cecac8995a8b1
رقم الأكسشن: edsdoj.fbb8bd8c8d3b4bd2995cecac8995a8b1
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14756366
14756374
DOI:10.1080/14756366.2022.2027933