Search results for "phosphonate"
showing 10 items of 372 documents
ChemInform Abstract: 2-Aryl-Substituted, Benzo-Anellated 5-Membered Heterocyclic Compounds as Potentially Active Substances for the Cardiovascular Sy…
2010
In the course of investigations on structure-activity relationships of calcium antagonists analogous to fostedil, a series of 2-aryl- and 2-arylvinyl-substituted 1,3-henzothiazoles and 1,3-benzoxazoles bearing a phosphonate group on the phenyl ring has been synthesized by cyclization, bromination, and subsequent Michaelis-Arbuzow reaction. Pharmacological investigations on isolated organs from guinea pigs revealed both negative inotropic effects and a relaxing action on smooth musculature; these activities were particularly pronounced in the 1,3-benzothiazole compound group.
2-Aryl-substituted, benzo-anellated 5-membered heterocyclic compounds as potentially active substances for the cardiovascular system: 1,3-Benzothiazo…
1992
In the course of investigations on structure-activity relationships of calcium antagonists analogous to fostedil, a series of 2-aryl- and 2-arylvinyl-substituted 1,3-henzothiazoles and 1,3-benzoxazoles bearing a phosphonate group on the phenyl ring has been synthesized by cyclization, bromination, and subsequent Michaelis-Arbuzow reaction. Pharmacological investigations on isolated organs from guinea pigs revealed both negative inotropic effects and a relaxing action on smooth musculature; these activities were particularly pronounced in the 1,3-benzothiazole compound group.
Gastrointestinal symptoms and association with medication use patterns, adherence, treatment satisfaction, quality of life, and resource use in osteo…
2016
The Medication Use Patterns, Treatment Satisfaction, and Inadequate Control of Osteoporosis Study (MUSIC-OS) is a prospective, observational study of women with osteoporosis in Europe and Canada. At baseline, patients with gastrointestinal symptoms reported lower adherence to osteoporosis treatment, treatment satisfaction, and health-related quality of life, than those without gastrointestinal symptoms. INTRODUCTION: The aim of the study was to examine gastrointestinal (GI) symptoms and the association between GI symptoms and treatment adherence, treatment satisfaction, and health-related quality of life (HRQoL) among osteoporotic women in Europe and Canada. METHODS: Baseline results are re…
Calcium binding and ionic conduction in single conical nanopores with polyacid chains: model and experiments.
2012
Calcium binding to fixed charge groups confined over nanoscale regions is relevant to ion equilibrium and transport in the ionic channels of the cell membranes and artificial nanopores. We present an experimental and theoretical description of the dissociation equilibrium and transport in a single conical nanopore functionalized with pH-sensitive carboxylic acid groups and phosphonic acid chains. Different phenomena are simultaneously present in this basic problem of physical and biophysical chemistry: (i) the divalent nature of the phosphonic acid groups fixed to the pore walls and the influence of the pH and calcium on the reversible dissociation equilibrium of these groups; (ii) the asym…
The dental management of patients at risk of medication-related osteonecrosis of the jaw: New paradigm of primary prevention
2018
Medication-related osteonecrosis of the jaw (MRONJ) is a serious adverse reaction of antiresorptive and antiangiogenic agents; it is a potentially painful and debilitating condition that can considerably affect the quality of life of patients. Furthermore, even if its epidemiology and pathogenesis have still not been fully clarified, several risk factors related to MRONJ have been recognized in prevention protocols. Three main risk factors are as follows: (i) the type of ONJ-related medications: antiresorptive (e.g., Bisphosphonates, Denosumab) and antiangiogenic drugs (e.g., Bevacizumab, Sunitinib); (ii) the category of patient at MRONJ risk: cancer versus non-cancer patient; (iii) the typ…
Phosphonylation Controls the Protein Corona of Multifunctional Polyglycerol-Modified Nanocarriers.
2018
Nanocarriers are a platform for modern drug delivery. In contact with blood, proteins adsorb to nanocarriers, altering their behavior in vivo. To reduce unspecific protein adsorption and unspecific cellular uptake, nanocarriers are modified with hydrophilic polymers like poly(ethylene glycol) (PEG). However, with PEG the attachment of further functional structures such as targeting units is limited. A method to introduce multifunctionality via polyglycerol (PG) while maintaining the hydrophilicity of PEG is introduced. Different amounts of negatively charged phosphonate groups (up to 29 mol%) are attached to the multifunctional PGs (Mn 2-4 kg mol-1 , Ð < 1.36) by post-modification. PGs are …
Synthesis of phosphono dipeptides, inhibitors of cathepsin C
1998
Abstract Phosphono dipeptides containing glycine, glycylglycine or L-alanine at N-termini and racemic phosphonic acid analogues of aromatic amino acids, as well as racemic alicyclic aminophosphonates, exhibit moderate inhibitory activity towards cathepsin C. This activity is probably due to the binding of the phosphonate moiety by a positively charged part of the enzyme which is complementary to the carboxylate part of the synthetic dipeptide products of the enzymatic reaction.
Analytical Methods Used in Biotransformation Studies of Organophosphonates
2022
This work was supported by the National Science Centre, Poland (NCN) grant number 2017/27/B/NZ4/00698. Among diverse organophosphorus compounds, whose residues are determined in various ecosystems, phosphonates possess special meaning. Regarding their biological activity, capability to chelating metal cations, and stability of direct carbon to phosphorus bond under physiological conditions, phosphonic compounds found many various applications. These compounds are commonly used as pesticides, drugs, anticorrosive agents, and additives to surfactants. Common use of these substances results in an increase in their concentration in various ecosystems which may cause considerable ecological prob…
Herbicidal derivatives of aminomethylenebisphosphonic acid. Part III. Structure-activity relationship.
1997
Derivatives of aminomethylenebisphosphonic acids constitute a class of promising herbicides. More than 40 N-substituted aminomethylenephosphonic acids were synthesized and evaluated for their herbicidal activity on common cress (Lepidium sativum L.) and cucumber (Cucumis sativus L.). Some of the tested compounds were found to exhibit strong herbicidal properties being equal in activity with the popular herbicide glyphosate as well as parent N-pyridylaminomethylenephosphonic acids. N-Substituted iminodi(methylenephosphonic) acids, which may be considered as close analog of glyphosate, were inactive toward test plants.
Inorganic Polyphosphate in Human Osteoblast-like Cells
1998
Significant amounts of inorganic polyphosphates and of polyphosphate-degrading exopolyphosphatase activity were detected in human mandibular-derived osteoblast-like cells. The amount of both soluble and insoluble long-chain polyphosphate in unstimulated osteoblast-like cells was higher than in human gingival cells, erythrocytes, peripheral blood mononuclear cells, and human blood plasma. The cellular content of polyphosphate in osteoblast-like cells strongly decreased after a combined treatment of the cells with the stimulators of osteoblast proliferation and differentiation, dexamethasone, beta-glycerophosphate, epidermal growth factor, and ascorbic acid. The amount of soluble long-chain p…