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.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8856110 | PMC |
| http://dx.doi.org/10.1080/14756366.2022.2027933 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Updates on Intrinsic Medicinal Chemistry of 1,4-dihydropyridines, Perspectives on Synthesis and Pharmacokinetics of Novel 1,4-dihydropyrimidines as Calcium Channel Blockers: Clinical Pharmacology.
Curr Top Med Chem
January 2025
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education & Research (JSS AHER), Mysuru, Karnataka, India.
Background: Several chemical studies described the physiological efficacy of 1,4- dihydropyridines (DHPs). DHPs bind to specific sites on the α1 subunit of L-type calcium channels, where they demonstrate a more pronounced inhibition of Ca2+ influx in vascular smooth muscle compared to myocardial tissue. This selective inhibition is the basis for their preferential vasodilatory action on peripheral and coronary arteries, a characteristic that underlies their therapeutic utility in managing hypertension and angina.
View Article and Find Full Text PDFSorghum grain as a bio-template: emerging, cost-effective, and metal-free synthesis of C-doped g-CN for photo-degradation of antibiotic, bisphenol A (BPA), and phenol under solar light irradiation.
Environ Sci Pollut Res Int
January 2025
Nano Photocatalysis Lab., Department of Chemistry, College of Science, Shiraz University, Shiraz, 7194684795, I.R. of Iran.
Due to the industry's rapid growth, the presence of organic pollutants, especially antibiotics, in water and wastewater resources is the main concern for wildlife and human health. Therefore, these days, a significant challenge is developing an efficient, sustainable, and eco-friendly photocatalyst. Natural biological models have numerous advantages compared to artificial model materials.
View Article and Find Full Text PDFAntennal sensilla variability among castes and sexes in the leaf-cutter ant Acromyrmex subterraneus subterraneus.
Protoplasma
January 2025
Departamento de Biologia Geral, Universidade Federal de Viçosa, Viçosa, MG, 36570-900, Brazil.
Insect antennae play a crucial role in communication, acting as receptors for both chemical and physical cues. This sensory reception is facilitated by specialized cuticular structures known as sensilla, which exhibit diverse morphologies and functions. In ants, caste polymorphism and sexual dimorphism manifest in antennal structure.
View Article and Find Full Text PDFGiant Seebeck Effect of Dibenzo[g,p]chrysene and its Derivatives: Deuteration and Substituent Effects and Relationship with Interlayer Distance.
Chem Asian J
January 2025
Kanagawa University, Department of Chemistry, JAPAN.
Thermoelectric properties of undoped crystals of dibenzo[g,p]chrysene (DBC), deuterated DBC (DBC-d16), and 2,10-dimethyl-DBC (DBC-Me2) have been studied to obtain some insights into the relationship between the structural parameters of materials and the giant Seebeck effect. X-ray crystallography showed one-dimensional columnar packing with the interlayer distances (d) for DBC-d16, DBC, and DBC-Me2 were 3.78 Å, 3.
View Article and Find Full Text PDF3D Printing Organogels with Bioderived Cyrene for High-Resolution Customized Hydrogel Structures.
Langmuir
January 2025
Surface Science and Bio-nanomaterials Laboratory, Department of Chemical Engineering, University of Waterloo, Waterloo, Ontario N2L 3G1 Canada.
3D printing techniques are increasingly being explored to produce hydrogels, versatile materials with a wide range of applications. While photopolymerization-based 3D printing can produce customized hydrogel shapes and intricate structures, its reliance on rigid printing conditions limits material properties compared to those of extrusion printing. To address this limitation, this study employed an alternative approach by printing an organogel precursor using vat polymerization with organic solvents instead of water, followed by solvent exchange after printing to create the final hydrogel material.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!