Search results for "phosphonate"
showing 10 items of 372 documents
Synthesis of fluorescent (benzyloxycarbonylamino)(aryl)methylphosphonates
2014
The synthesis of a library of structurally variable aromatic esters of (benzyloxycarbonylamino)(aryl)methylphosphonic acids is described by means of the Oleksyszyn reaction. The library was enlarged by the application of a Suzuki–Miayra approach and by preparation of mixed esters.
α-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine- and neutral a…
2005
Abstract The synthesis and biological activity studies of the series of structurally different α-aminoalkylphosphonates were performed in order to optimise the shape of the side chain of the potential inhibitors in S1 pocket of leucine aminopeptidase [E.C.3.4.11.1]. Analysis of a series of compounds with aromatic, aliphatic and alicyclic P1 side chains enabled to find out the structural features, optimal for that fragment of inhibitors of LAP. The most active among all investigated compounds were the phosphonic analogues of homo-tyrosine ( K i = 120 nM) and homo-phenylalanine ( K i = 140 nM), which even as racemic mixtures were better inhibitors in comparison with the best till now-phosph…
Dipeptide analogues of fluorinated aminophosphonic acid sodium salts as moderate competitive inhibitors of cathepsin C
2023
In this paper, we present the solvolysis reaction of dipeptide analogues of fluorinated aminophosphonates with simultaneous quantitative deprotection of the amino group. To the best of our knowledge, this work is the first reported example of the application of fluorinated aminophosphonates in cathepsin C inhibition studies. The new molecules show moderate inhibition of the cathepsin C enzyme, which opens the door to consider them as potential therapeutic agents. Overall, our findings provide a new avenue for the development of fluorinated aminophosphonate-based inhibitors. This article is part of the thematic issue "Organophosphorus chemistry: from model to application".
Separation of aminoalkanephosphonic acid enantiomers by indirect UV detection capillary electrophoresis with application of cyclodextrins.
2003
Indirect UV detection capillary electrophoresis (CE) was used for the separation of aminoalkanephosphonic acid (AP) enantiomers by applying commercially available cyclodextrins as chiral discriminators. The results show that the separation of the enantiomers depends on pH of the background electrolyte, the molar ratio of cyclodextrin to aminophosphonic acid, and on the type of the applied chiral selector. Optimization of process conditions allowed enantiomeric baseline separation or partial separation of 12 out of 14 alpha-aminophosphonic acids studied. This type of CE might therefore be successfully used for routine determination of enantiomeric purity of aminophosphonic acids.
BIODEGRADACJA ZWIĄZKÓW FOSFONOWYCH PRZEZ GRZYBY
2020
Phosphonates are the group of organophosphorus compounds, which are characterized by the presence of covalent bond(s) between carbon and phosphorus atom in their structure. Both; the natural and synthetic phosphonic compounds, are encountered in various ecosystems, however because of their wide range of applications, the latter ones are considerably more frequently discussed. Regarding the broad spectrum of biological activity, capability to chelate metal cations and environmental stability of direct carbon to phosphorus bond under physiological conditions, phosphonic compounds found a variety of applications e.g. as pesticides, drugs, anticorrosive agents, additives to surfactants and flam…
Significance of immunohistochemistry biomarkers in prediction of malignant transformation of oral lichen planus
2022
Background: Oral lichen planus (OLP) is a chronic inflammatory disorder with increased risk for malignant transformation. Biomarker validation is a pivotal step in moving newly discovered biomarkers towards clinical implementation. We performed a systematic review of studies on biomarkers related to OLP, wherein biomarkers have been described in at least two independent studies. Our aim was to determine whether any of these biomark-ers might be promising in predicting the increased risk of malignant transformation of OLP. Material and Methods: We searched the following databases until August 2021: PUBMED, EMBASE, and Web of Science. Due to high heterogeneity, a qualitative rather than quant…
Potentiation of the cytotoxic activity of copper by polyphosphate on biofilm-producing bacteria: A bioinspired approach
2012
Adhesion and accumulation of organic molecules represent an ecologically and economically massive problem. Adhesion of organic molecules is followed by microorganisms, unicellular organisms and plants together with their secreted soluble and structure-associated byproducts, which damage unprotected surfaces of submerged marine structures, including ship hulls and heat exchangers of power plants. This is termed biofouling. The search for less toxic anti-biofilm strategies has intensified since the ban of efficient and cost-effective anti-fouling paints, enriched with the organotin compound tributyltin, not least because of our finding of the ubiquitous toxic/pro-apoptotic effects displayed b…
Medication-Related Osteonecrosis of Jaws (MRONJ) Prevention and Diagnosis: Italian Consensus Update 2020
2020
The Medication-Related Osteonecrosis of Jaws (MRONJ) diagnosis process and its prevention play a role of great and rising importance, not only on the Quality of Life (QoL) of patients, but also on the decision-making process by the majority of dentists and oral surgeons involved in MRONJ prevention (primary and secondary). The present paper reports the update of the conclusions from the Consensus Conference—held at the Symposium of the Italian Society of Oral Pathology and Medicine (SIPMO) (20 October 2018, Ancona, Italy)—after the newest recommendations (2020) on MRONJ were published by two scientific societies (Italian Societies of Maxillofacial Surgery and Oral Pathology and Medicine, SI…
Crystal structure of zwitterionic 3-(2-hydroxy-2-phosphonato-2-phosphonoethyl)imidazo[1,2-a]pyridin-1-ium monohydrate (minodronic acid monohydrate): …
2014
A redetermination of the crystal structure of minodronic acid monohydrate was carried out in order to provide accurate atomic coordinates and geometry information, whose knowledge is fundamental to elucidate the presumed polymorphism of the compound at room temperature.
Bone Density, Balance and Quality of Life of Postmenopausal Women Taking Alendronate Participating in Different Physical Activity Programs
2010
Made available in DSpace on 2022-04-28T19:04:59Z (GMT). No. of bitstreams: 0 Previous issue date: 2010-01-01 Background: The objective of this study was to determine the effects of different physical activity (PA) programs on bone density, balance and quality of life of postmenopausal women taking concomitant alendronate. A quasi-experimental study was conducted with 35 volunteers divided into four groups: practitioners of resistance training (RTG, n = 9, 49.8±4.2 years), judo (JUG, n = 11, 52.2±5.3 years), water aerobics (WAG, n = 8, 57.1±7.4 years) and the control group (CG, n = 7, 53.8±4.4 years). Methods: The following assessment tools were used: bone mineral density (BMD) measured by d…