Search results for "dipeptide"
showing 10 items of 99 documents
Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation.
2015
Novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation were developed; some of them possess K(i) values in the micromolar range. We studied the structure-activity relationship of these derivatives and we performed docking studies, which allowed us to find out the key interactions established by the inhibitors with the target enzyme. Biological results indicate that the nature of the P2 and P3 substituents and their binding to the S2/S3 pockets is strictly interdependent.
Synthesis and spectroscopic characterization of dicyclohexyltin derivatives of dipeptides, andin vitro effects against MDA-MB 231 breast cancer cells…
1992
Dicyclohexyltin derivatives Cy2SnL (Cy = cyclohexyl) of the dipeptides H2L, glycylglycine, glycylalanine, alanylglycine, glycylvaline, glycylmethionine, glycylphenylalanine and glycyltyrosine, have been obtained by neutralization of Cy2SnO and H2L. The crystal structures of Cy2SnL (L = glycylglycinate, glycylalaninate) have been determined by single X-ray diffraction. Tin in each case has a distorted trigonal bipyramidal environment with the dipeptide acting as a tridentate NNO-ligand. From IR-data, and in some cases from 119Sn Mossbauer and 119Sn NMR data, analogous molecular structures are inferred for the other compounds Cy2SnL. Spectroscopic data indicate that the solid-state structures…
Semi-empirical MNDO study of the structure of some diorganotin (IV) glycylglycinates
1993
The geometrical structures of some diorganotin glycylglycinates have been obtained using the MNDO semi-empirical method. A good agreement with the experimental diffractometric data was found.
Conformational Analysis of beta-Lactam-Containing Ferrocene Peptides
2009
The homochiral 3-amino-1-(4-methoxyphenyl)-4-phenyl-beta-lactam (≡ Alm) was conjugated with Boc-Ala giving Ala-Alm (9) after Boc-deprotection (Boc = tert-butoxycarbonyl, Ala = alanine). Coupling of FcCOOH (1) and Boc-Fca (10) with “ dipeptide” 9 resulted in the formation of FcCO-Ala-Alm (12) and the trisamide Boc-Fca-Ala-Alm (13), respectively (Fc = ferrocenyl, Fca = 1’ -aminoferrocene-1-carboxylic acid). The reactions were accomplished by the HOBt/EDC procedure and the products were obtained in good yields (HOBt = 1-hydroxybenzotriazole, EDC = N-(3-dimethylaminopropyl)-N’ -ethylcarbodiimide hydrochloride). Symmetrically 1, 1’ -disubstituted “ tetrapeptide” Fn(CO-Ala-Alm)2 (14) was prepared…
Comparative Study of the Effects Exerted by N-Valproyl-L-Phenylalanine and N-valproyl-L-tryptophan on CA1 Hippocampal Epileptiform Activity in Rat
2018
Background: The research on the improvement of epilepsy therapy is constantly growing. Valproyl-LPhenylalanine (VPA-Phen) and N-valproyl-L-tryptophan (VPA-Tryp) were synthesized to increase the antiepileptic efficacy of valproic acid. Methods: VPA-Phen and VPA-Tryp were comparatively tested on CA1 hippocampal epileptiform bursting activity obtained by increasing potassium and lowering calcium and magnesium concentrations in the fluid perfusing rat brain slices. Each slice was treated with a single concentration (0.2, 0.5, 1 mM) of VPA-Phen or VPA-Tryp. Both burst duration and interburst frequency, during and after treatment, were off-line compared with baseline values. For both parameters,…
Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors
2011
The multiligand Receptor for Advanced Glycation End products (RAGE) is involved in various pathophysiological processes, including diabetic inflammatory conditions and Alzheimers disease. Full-length RAGE, a cell surface-located type I membrane protein, can proteolytically be converted by metalloproteinases ADAM10 and MMP9 into a soluble RAGE form. Moreover, administration of recombinant soluble RAGE suppresses activation of cell surface-located RAGE by trapping RAGE ligands. Therefore stimulation of RAGE shedding might have a therapeutic value regarding inflammatory diseases. We aimed to investigate whether RAGE shedding is inducible via ligand-induced activation of G protein-coupled recep…
Inhibitory effects of N-valproyl-L-tryptophan on high potassium, low calcium and low magnesium-induced CA1 hippocampal epileptiform bursting activity…
2012
N-valproyl-l-tryptophan (VPA-Tryp), new antiepileptic drug, was tested on CA1 hippocampal epileptiform bursting activity obtained by increasing potassium and lowering calcium and magnesium concentrations in the fluid perfusing rat brain slices. Each slice was treated with a single concentration (0.2, 0.5, 1 or 2 mM) of Valproate (VPA) or VPA-Tryp. Both burst duration and interburst frequency during and after treatment were off-line compared with baseline values. For both parameters, the latency and the length of statistically significant response periods as well as the magnitude of drug-induced responses were calculated. VPA-Tryp evoked fewer and weaker early excitatory effects than VPA on …
Kidney donors and kidney transplants have abnormal aminothiol redox status, and are at increased risk of oxidative stress and reduced redox buffer ca…
2013
Abstract Objective Living kidney donors have been part of a successful kidney transplant programme in Norway for almost 50 years. Glomerular filtration rates (GFRs) have tended to remain stable at about 70% of pre-donation levels. Plasma total homocysteine (Hcy) has an inverse relationship to kidney function, and previous reports indicate elevated levels of Hcy in kidney donors. We wanted to examine the most important plasma aminothiols in kidney donors, i.e. Hcy, cysteine (Cys) and cysteinylglycine (CG) with their redox species. The aminothiol redox-system appears to be an integral part of the extracellular antioxidant defence system in the body. Design and methods Plasma concentrations of…
Decreased level of cardiac antioxidants in endurance-trained rats.
1989
Han-Wistar rats were exposed to a 194-200 h swimming protocol which caused a significant increase in the cardiac weight. The levels of various tissue antioxidants were assayed from the myocardium of the right ventricle and from the left ventricle (subendo- and subepimyocardium). This endurance training decreased the activities of catalase in the right ventricle and in the subendo- and subepimyocardium and Cu,Zn-superoxide dismutase in the subendomyocardium as well as the concentration of vitamin E in the right ventricle and in the subendomyocardium. Also, the activity of thioredoxin reductase decreased in each part of myocardium and that of glutathione reductase in the right ventricle and i…
Sequential Treatment Escalation with Dapagliflozin and Saxagliptin Improves Beta Cell Function in Type 2 Diabetic Patients on Previous Metformin Trea…
2018
AbstractWe investigated the effect of sequential treatment escalation with dapagliflozin and saxagliptin on beta cell function in patients with T2DM insufficiently controlled on metformin monotherapy during a hyperglycaemic clamp investigation. Twenty-six patients (19 males, age 63.5±7.0 years; duration of diabetes 8.8±4.7 years; HbA1c 63.9±15.8 mmol/mol; mean±SD) were enrolled in the study. During a first treatment period (TP1) all patients received 10 mg dapagliflozin for one month, followed by the addition of 5 mg saxagliptin or placebo for another month (TP2). At baseline and at the end of each treatment period, fasting glucose and insulin levels were analysed, and a hyperglycaemic clam…