The article deals with the hydrophobic character (distribution coefficient in the systems hexane - water and chloroform - water) and certain peculiarities of distributing three cation-containing phosphoroganic inhibitors of cholinesterase and their uncharged analogues in the organisms. The distribution coefficients in the charged and uncharged compounds in the system hexane - water differ inconsiderably, whereas in the system chloroform-water by the thousands and millions times. In rabbits with intravenous administration the content of all inhibitors in blood decreases rapidly, the uncharged compounds accumulate selectively in the lungs and the charged ones are distributed evenly in the tissues.
Download full-text PDF |
Source |
---|
Biomolecules
October 2024
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Trg Marka Marulića 19, HR-10 000 Zagreb, Croatia.
In previous research, 1,2,3-triazolium salts showed significant biological activity as potential inhibitors of cholinesterase enzymes (ChEs), which are crucial for neurotransmission. In this research, pairs of uncharged thienobenzo-triazoles and their charged salts were prepared in order to further examine the role of the positive charge on the nitrogen of the triazole ring in interactions within the active site of the enzymes, and to compare the selectivity of 1,2,3-triazolium salts in relation to their uncharged analogs obtained by photochemical cyclization. Neutral thienobenzo-triazoles showed very good selective activity toward butyrylcholinesterase (BChE), while their salts showed excellent non-selective inhibition toward both BChE (the most active : IC 0.
View Article and Find Full Text PDFMacromol Rapid Commun
December 2024
Institute of Sustainability for Chemicals, Energy and Environment (ISCE2), Agency for Science, Technology and Research (A*STAR), 1, Pesek Road, Jurong Island, Singapore, 627833, Singapore.
Int J Pharm
October 2024
Department of Medicinal Chemistry, Uppsala University, SE-75123 Uppsala, Sweden. Electronic address:
Subcutaneous (SC) injection is a common route of administration for drug compounds with poor oral bioavailability. However, bioavailability is often variable and incomplete, and there is as yet no standard accepted medium for simulation of the human SC environment. In this work we evaluate a FRAP based method for quantitative determination of local self-diffusion coefficients within extracellular matrix (ECM) mimetic hydrogels, potentially useful as in vitro models for drug transport in the ECM after SC injection.
View Article and Find Full Text PDFJ Cell Biochem
September 2024
Molecular Bio-Computation and Drug Design Research Group, School of Health Sciences, University of KwaZulu Natal, Westville Campus, Durban, South Africa.
Protein-protein interactions, or PPIs, are a part of every biological activity and have been linked to a number of diseases, including cancer, infectious diseases, and neurological disorders. As such, targeting PPIs is considered a strategic and vital approach in the development of new medications. Nonetheless, the wide and flat contact interface makes it difficult to find small-molecule PP inhibitors.
View Article and Find Full Text PDFOrg Biomol Chem
August 2024
Department of Chemistry, Indian Institute of Science Education and Research (IISER) Pune, Dr Homi Bhabha Road, Pune 411008, India.
Nucleic acids (DNA and RNA) can form diverse secondary structures ranging from hairpins to duplex, triplex, G4-tetraplex and C4-i-motifs. Many of the DNA analogues designed as antisense oligonucleotides (ASO) are also adept at embracing such folded structures, although to different extents with altered stabilities. One such analogue, peptide nucleic acid (PNA), which is uncharged and achiral, forms hybrids with complementary DNA/RNA with greater stability and specificity than DNA:DNA/RNA hybrids.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!