Search results for "Amidine"

Thioredoxin (Trxo1) interacts with proliferating cell nuclear antigen (PCNA) and its overexpression affects the growth of tobacco cell culture.

2017

Thioredoxins (Trxs), key components of cellular redox regulation, act by controlling the redox status of many target proteins, and have been shown to play an essential role in cell survival and growth. The presence of a Trx system in the nucleus has received little attention in plants, and the nuclear targets of plant Trxs have not been conclusively identified. Thus, very little is known about the function of Trxs in this cellular compartment. Previously, we studied the intracellular localization of PsTrxo1 and confirmed its presence in mitochondria and, interestingly, in the nucleus under standard growth conditions. In investigating the nuclear function of PsTrxo1 we identified proliferati…

In silico discovery of substituted pyrido[2,3-d]pyrimidines and pentamidine-like compounds with biological activity in myotonic dystrophy models

2016

Myotonic dystrophy type 1 (DM1) is a rare multisystemic disorder associated with an expansion of CUG repeats in mutant DMPK (dystrophia myotonica protein kinase) transcripts; the main effect of these expansions is the induction of pre-mRNA splicing defects by sequestering muscleblind-like family proteins (e.g. MBNL1). Disruption of the CUG repeats and the MBNL1 protein complex has been established as the best therapeutic approach for DM1, hence two main strategies have been proposed: targeted degradation of mutant DMPK transcripts and the development of CUG-binding molecules that prevent MBNL1 sequestration. Herein, suitable CUG-binding small molecules were selected using in silico approach…

Search of Chemical Scaffolds for Novel Antituberculosis Agents

2005

3 A method to identify chemical scaffolds potentially active against Mycobacterium tuberculosis is presented. The molecular features of a set of structurally heterogeneous antituberculosis drugs were coded by means of structural invariants. Three tech- niques were used to obtain equations able to model the antituberculosis activity: linear discriminant analysis, multilinear re- gression, and shrinkage estimation-ridge regression. The model obtained was statistically validated through leave-n-out test, and an external set and was applied to a database for the search of new active agents. The selected compounds were assayed in vitro, and among those identified as active stand reserpine, N,N,N…

Topical Voriconazole as Supplemental Treatment for Acanthamoeba Keratitis

2020

Purpose Voriconazole was shown to inhibit ergosterol synthesis in various acanthamoeba species. The purpose of this study was to evaluate the clinical outcome of treatment with supplemental topical voriconazole in patients with acanthamoeba keratitis (AK). Methods All patients who had been treated for AK with voriconazole 1% drops in conjunction with topical first-line antiacanthamoeba therapy composed of polyhexamethylene biguanide (PHMB) 0.02% and propamidine isethionate 0.1% (Brolene) between November 2014 and August 2017 at the Department of Ophthalmology, University Medical Center Mainz, were included. The main outcomes were treatment failure and recurrence rate. Secondary outcomes wer…

Moderate intake of n-3 fatty acids is associated with stable erythrocyte resistance to oxidative stress in hypertriglyceridemic subjects.

2001

Background The important triacylglycerol-lowering capacity of n-3 fatty acids is counterbalanced by their inherent sensitivity to oxidation. Inconsistent results about the latter have been reported in hypertriglyceridemic individuals. After incorporation into cell membranes, n-3 fatty acids may alter membrane-related functions. In view of the distinct composition of hypertriglyceridemic membranes and the prooxidant status in this condition, it can be surmised that cell enrichment with the oxidizable n-3 fatty acids will be associated with an increased hemolytic process. Objective We sought to evaluate the effect of fish oil consumption on n-3 fatty acid incorporation into erythrocyte membra…

Darstellung und H2-agonistische Aktivität alkylsubstituierter 3-(Imidazol-4-yl)propylguanidine Synthesis and H2-Agonistic Activity of Alkyl-3-(imidaz…

1987

Derivate des 3-(Imidazol-4-yl)propylguanidins mit einem Methyl- oder einem 2-(Ethylthio)ethyl-Substituenten2) an der Guanidin-Gruppe weisen am H2-Rezeptor des Meerschweinchenvorhofs nur 10–20% der Histaminaktivitat auf. Dagegen fuhrt die Substitution mit der H2-affinen 2-[(5-Methylimidazol-4-yl) methylthio]ethyl-Gruppierung zu Impromidin, einem hochpotenten H2-Agonisten.

Cover Picture: A Versatile Approach to CF3-Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis of Amid…

2015

Histaminanaloge, 28. Mitt. 2-Aryloxyalkyl- und 2-Aminoalkylhistamine

1987

Als Histaminderivate mit H1-affinitatsvermittelnden Strukturelementen in 2-Stellung des Imidazolrings wurden 2-Aryloxyalkyl- und 2-Aminoalkylhistamine sowie das racemische 2-(1-Phenylethyl)histamin dargestellt und auf Histamin-H1-agonistische Aktivitat untersucht. Histamine Analogues, XXVIII: 2-(Aryloxyalkyl)- and 2-(Aminoalkyl)histamines As histamine derivatives with structures at position 2 of the imidazole ring, which mediate H1-receptor affinity, 2-(aryloxyalkyl)- and 2-(aminoalkyl)histamines as well as racemic 2-(1-phenylethyl)histamine were prepared and tested for histamine H1-agonistic activity.

Pentafulvene durch Aminomethinylierung des Cyclopentadiens

1986

Aus der Dreikomponentenreaktion von Cyclopentadien (1) mit s-Triazin (2) und einem sekundaren Amin 4 gehen die cyclisch N,N-disubstituierten Pentafulven-6-amine 5 und die cyclisch N1,N1-disubstituierten N2-(6-Pentafulvenyl)formamidine 7 hervor. Unter den biologischen Eigenschaften der neuen Verbindungen ist besonders die anthelminthische Wirkung von 5d interessant. Pentafulvenes by Aminomethynylation of Cyclopentadiene The three component reaction comprising the interaction of cyclopentadiene (1) with s-triazine (2) and a secondary amine 4 leads to the cyclic N,N-disubstituted pentafulven-6-amines 5 and the cyclic N1,N1-disubstituted N2-(6-pentafulvenyl)formamidines 7. Among the biological …

ChemInform Abstract: A Versatile Approach to CF3-Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis o…

2016

The synthesis of new fluorinated pyrrolidones starting from unprotected amino esters and amino nitriles through a Michael addition-lactamization sequence is described. The resulting CF3 -containing building blocks, bearing a quaternary stereogenic center adjacent to the fluorinated group, have been converted into amino pyrrolidines that display potent β-secretase 1 (BACE1) inhibitory activity. This work constitutes an example of selective fluorination as a valid strategy for the modulation of physicochemical and biological properties of lead compounds in drug discovery.