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Amidines (4):
Recent article
Amidines
Biomacromolecules (12)9 2011
Abstract
We investigated the properties of micellar siRNA delivery vehicles prepared with poly(ethylene glycol)-block-poly(l-lysine) (PEG-b-PLL) comprising lysine amines modified to contain amidine and thiol functionality. Lysine modification was achieved using 2-iminothiolane (2-IT) [yielding PEG-b-PLL(N2IM...
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PMID: 21863796
PDF is available here.
PDF is available here.
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Abstract
We studied cation selectivity by outward-facing sites (high K(+) affinity) of Na/K pumps expressed in Xenopus oocytes, under voltage clamp. Guanidinium(+), methylguanidinium(+), and aminoguanidinium(+) produced two phenomena possibly reflecting actions at site III: (i) voltage-dependent inhibition (...
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PMID: 20937860
PDF is available here.
PDF is available here.
Abstract
We detected a strongly catecholaminergic character and in majority neuropeptide Y (NPY)-positive staining of the colon-projecting FB+ neurons both in the control and the inflamed animals. Furthermore, colonic inflammation caused the significant increase in density of galanin- (P<0.001), somatostatin...
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PMID: 20460841
PDF is available here.
PDF is available here.
Abstract
To investigate the AAPH scavenging activities of 22 flavonoids and phenolic acids and 9 extracts of Chinese materia medica.
The antioxidant activities of the samples were evaluated by an oxygen radical absorbance capacity method (ORAC), at the same time, the total contents of flavonoids and phenolic...
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PMID: 21137342
PDF is available here.
PDF is available here.
Chemical Communications (46)31 2010
Abstract
In contrast to amidines bearing ionizable alpha-CH bonds, which react with nitric oxide (NO) to add diazeniumdiolate groups at their alpha-carbons, benzamidine forms an N-bound diazeniumdiolate that can be further derivatized at the other amidine nitrogen and/or the terminal oxygen to form caged NO...
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PMID: 20589293
PDF is available here.
PDF is available here.
Abstract
The title compound, N,N'-di(2-methoxyphenyl)formamidine (DMPF) was synthesized and characterized by FT-IR, FT-Raman, (1)H NMR, (13)C NMR spectroscopy and X-ray single crystal diffraction. The results show that the compound crystallizes in an orthorhombic system, with space group of Pbca and eight mo...
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PMID: 20409749
PDF is available here.
PDF is available here.
Cerebral Cortex (20)7 2010
Abstract
We looked for reciprocal projections from visual cortex to caudal auditory cortical areas in macaque monkeys. We found direct projections from area prostriata and the peripheral visual representations of area V2. Projections were more abundant after injections of temporoparietal area and caudal para...
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PMID: 19875677
PDF is available here.
PDF is available here.
Physical Review Letters (104)22 2010
Abstract
Direct force measurements between oppositely charged latex particles in aqueous electrolyte solutions were carried out with a multiparticle colloidal probe technique based on atomic force microscopy. Force profiles between two dissimilarly charged surfaces can be only described when charge regulatio...
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PMID: 20867210
PDF is available here.
PDF is available here.
Abstract
4-methyl-8-hydroxylpsoralen (MXan) and 4,9-dimethyl-8-hydroxylpsoralen (DMXan) were synthesized in order to clarify the effect of methyl on the antioxidant effectiveness of xanthotoxol (8-hydroxylpsoralen, Xan), which were assessed by bleaching beta-carotene in linoleic acid-Triton emulsion, by inte...
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PMID: 20332056
PDF is available here.
PDF is available here.
Abstract
We determined the ability of extracts and active components isolated from nine medicinal plants, Poncirus trifoliata, Astragalus membranaceus, Magnolia obovata, Salvia miltiorrhiza, Angelica dahurica, Cornus officinalis, Cnidium officinale, Pueraria lobata and Ostericum koreanum, to neutralize perox...
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PMID: 20607491
PDF is available here.
PDF is available here.
Abstract
We provide evidence that lipophilicity and not only radical scavenger potency is an important factor regarding the efficiency of antihemolytic substances....
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PMID: 20397726
PDF is available here.
PDF is available here.
Abstract
N'-cyanoisonicotinamidine derivatives, linked to an arylpiperazine moiety, were prepared to identify highly selective and potent 5-HT(1A) ligands as potential pharmacological tools in studies of wide spread psychiatric disorders. The combination of structural elements (heterocyclic nucleus, alkyl ch...
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PMID: 20347301
PDF is available here.
PDF is available here.
Abstract
There exists an urgent need to develop licensed drugs and vaccines for the treatment or prevention of filovirus infections. FGI-103 is a low-molecular-weight compound that was discovered through an in vitro screening assay utilizing a variant of Zaire ebolavirus (ZEBOV) that expresses green fluoresc...
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PMID: 20211898
PDF is available here.
PDF is available here.
Biological Psychiatry (67)9 2010
Neuroplasticity in the mesolimbic system induced by natural reward and subsequent reward abstinence.
Abstract
Sexual experience induces functional and morphological alterations in the mesolimbic system similar to repeated exposure to psychostimulants. Moreover, abstinence from sexual behavior after repeated mating was essential for increased reward for drugs and dendritic arbors of NAc neurons, suggesting t...
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PMID: 20015481
PDF is available here.
PDF is available here.
Amino Acids (38)4 2010
Abstract
We should think about clays not just sink of molecules, but as primitive vessels of production of biomolecules. At pH 8.00, an increasing expansion was observed in the following order for both minerals: thiourea > thiocyanate > cysteine. At pH 3.00, the same order was not observed and thiourea had a...
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PMID: 19579002
PDF is available here.
PDF is available here.
Abstract
We demonstrate that Hsps play an important role in the regulation of initiation of protein synthesis during oxidative stress....
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PMID: 20521618
PDF is available here.
PDF is available here.
Journal of Neurosurgery (112)4 2010
Abstract
The hypothesis that significant motoneuron cell death occurs after chronic and or sequential nerve injury was rejected. Despite cell survival, only 50% of motoneurons are capable of exhibiting a regenerative response, consistent with our previous findings of reduced regeneration after chronic axotom...
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PMID: 19764828
PDF is available here.
PDF is available here.
Abstract
Heterocyclic amidine derivatives have been synthesized by condensation of 2-cyanopyrazine, 4-cyanopyridine and 2-cyanopyridine with furfurylamine, histamine, 1-(3-aminopropyl)imidazole, 4-picolylamine, 2-picolylamine, and tryptamine respectively, in the presence of sodium methoxide as well as via mi...
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PMID: 19959259
PDF is available here.
PDF is available here.
Thrombosis and Haemostasis (103)3 2010
Abstract
AZD0837 is an investigational oral anticoagulant which is converted to the active form, AR-H067637, a selective direct thrombin inhibitor. The present study, a multicentre, randomised, parallel-group, dose-guiding study, assessed the safety and tolerability of an immediate-release formulation of AZD...
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PMID: 20076850
PDF is available here.
PDF is available here.
Parasitology (137)2 2010
Abstract
Our data provide further information regarding the activity of this class of compounds upon T. cruzi which should aid future design and synthesis of agents that could be used for Chagas disease therapy....
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PMID: 19765349
PDF is available here.
PDF is available here.
Abstract
These results emphasize that the residue situation is clearly underestimated if only the parent compound is targeted, and they reinforce how important it is to include amitraz in the target scope of pesticide residue laboratories, especially since the concentrations detected exceeded the Acute Refer...
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PMID: 20480882
PDF is available here.
PDF is available here.
Abstract
The reactions of N-(5,6,7,8-tetrahydroquinazolin-4-yl)amidines and their amide oximes with hydroxylamine hydrochloride gave abnormal cyclization products via a ring cleavage of pyrimidine component accompanied with a ring closure of 1,2,4-oxadiazole to give N-[2-([1,2,4]oxadiazol-5-yl)cyclohexen-1-y...
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PMID: 20190443
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (60)6 2010
Abstract
Isolated rat mesenteric arteries were incubated with lipopolysaccharide (LPS) for 6 h and then mounted in an organ bath to investigate their responses to various relaxants. Exposure to LPS moderately reduced acetylcholine (ACh)-induced endothelium-dependent relaxation (EDR), and markedly reduced sod...
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PMID: 20648920
PDF is available here.
PDF is available here.
Abstract
We used 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH), a water-soluble generator of peroxyl and alkoxyl radicals, to investigate the susceptibility of CS to oxidative damage. Treatment of isolated mitochondria with AAPH for 8-24 h led to CS inactivation; however, the activity of aconitase, a...
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PMID: 19795928
PDF is available here.
PDF is available here.
Abstract
Our findings clearly show a novel antioxidant role for caffeic acid and quercetin at the adipose tissue level. These new data confirm the beneficial role of phytotherapy as an interesting alternative mean for the development of novel therapeutical and nutritional strategy to prevent metabolic disord...
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PMID: 19152116
PDF is available here.
PDF is available here.
Nanotechnology (20)45 2009
Abstract
We used electron spin resonance to quantify the residual peroxyl radical ([Formula: see text]) generated from 2,2-azobis (2-aminopropane) dihydrochloride (AAPH) by thermal decomposition in the presence of O(2) and a spectrophotometric method to quantify the residual 1,1-diphenyl-2-picrylhydrazyl (DP...
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PMID: 19834242
PDF is available here.
PDF is available here.
Folia morphologica (68)4 2009
Abstract
We hypothesized that an increase in intracellular NADH using specific substrates will protect RL-34 cells against cytotoxicity of 2'-azobis (2-amidinopropane) dihydrochloride (AAPH), which is a peroxyl radical generating compound. Cells treated for 24 hours with 6.0 mM AAPH were severely damaged: mi...
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PMID: 19950075
PDF is available here.
PDF is available here.
Journal of Neurotrauma (26)10 2009
Abstract
We employed Fast Blue (FB) axonal tracing to determine the origin of regenerating axons after thoracic spinal cord transection injury in rats. Schwann cell (SC)-loaded, biodegradable, poly(lactic-co-glycolic acid) (PLGA) scaffolds were implanted after transection. Scaffolds loaded with solubilized b...
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PMID: 19413501
PDF is available here.
PDF is available here.
Biochemistry (Washington) (48)36 2009
Abstract
Molecules that block nitric oxide's (NO) biosynthesis are of significant interest. For example, nitric oxide synthase (NOS) inhibitors have been suggested as antitumor therapeutics, as have inhibitors of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme that catabolizes endogenous NOS inhibi...
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PMID: 19663506
PDF is available here.
PDF is available here.
Biochemistry (Washington) (48)35 2009
Abstract
We propose that similar priming mechanisms may contribute to the unexpected platelet-activating effects of pharmaceutical integrin antagonists....
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PMID: 19640007
PDF is available here.
PDF is available here.
Abstract
The direction of dehydrogenation with Hg(II)-EDTA of 2-substituted pyrrolidines and piperidines is examined at the model substances 1-4 featuring a N-(2-amino-2-phenylethyl) substituent, which is able to capture an iminium intermediate. Compounds 1-4 represent mixtures of diastereomers; the separati...
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PMID: 19827296
PDF is available here.
PDF is available here.
Journal of Organic Chemistry (74)15 2009
Abstract
CuI/L5 (N,N'-dimethylethylenediamine) proves to be an efficient catalyst system for the amination of arylhalides with guanidines. The same catalyst system is then successfully applied to the one-step synthesis of 1-H-2-amino-benzimidazoles through tandem aminations of 1,2-dihaloarenes in modest yiel...
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PMID: 19527012
PDF is available here.
PDF is available here.
Abstract
We studied the free radical generation involved in the development of interstitial pneumonia (IP) in an animal model of autoimmune disease. We observed an electron spin resonance (ESR) spectrum of alpha-(4-pyridyl-1-oxide)-N-tert-butylnitrone (POBN) radical adducts detected in the lipid extract of l...
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PMID: 19376221
PDF is available here.
PDF is available here.
Abstract
We hypothesized that diabetes induces PP2B-dependent upregulation of NOS activity and NO production in the mTAL. Three weeks after injection of streptozotocin (STZ rats) or vehicle (sham rats), mTAL suspensions were prepared for use in functional and biochemical assays. PP2B activity and expression...
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PMID: 19458119
PDF is available here.
PDF is available here.
Abstract
To explore the toxicity of LPS-induced activated microglia to preoligodendrocytes (preOLs) and the effect of 1400W, a selective inhibitor of inducible nitric oxide synthetase (iNOS), on the blockage of the toxicity.
Co-cultured microglia and preOLs obtained from two-day-old Sprague-Dawley (SD) rats...
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PMID: 19951519
PDF is available here.
PDF is available here.
Analytical Biochemistry (390)1 2009
Abstract
We report here a cellular model for screening NOS inhibitors. Stable transformants were generated by overexpressing rat neuronal NOS in HEK 293T cells. The enzyme was activated by introducing calcium ions into cells, and its activity was assayed by determining the amount of nitrite that was formed i...
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PMID: 19362065
PDF is available here.
PDF is available here.
Thrombosis and Haemostasis (101)6 2009
Abstract
AZD0837 is in development as a new oral anticoagulant for use in thromboembolic disorders. In vivo, AZD0837 is converted to AR-H067637, a selective and reversible direct thrombin inhibitor. Established biochemical methods were used to assess and measure the biochemical and pharmacological properties...
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PMID: 19492147
PDF is available here.
PDF is available here.
Abstract
The antioxidant effects of alpha-terpinene (alpha-TH) and gamma-terpinene (gamma-TH) on the oxidation of methyl linoleate (LH), DNA, and erythrocytes induced by 2,2'-azobis(2-amidinopropane hydrochloride) (AAPH) were investigated. The results from erythrocytes and DNA were treated by means of chemic...
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PMID: 19326866
PDF is available here.
PDF is available here.
Anticancer Research (29)4 2009
Abstract
Cytotoxic activity of DOX toward HL60/MX2 cells was about 195 times lower when compared with the sensitive HL60 cell line. DOXM and DOXH were approximately 20 times more active in resistant cells than DOX. It was found that the uptake of DOX was lower in resistant cells by about 16%, while that of D...
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PMID: 19414398
PDF is available here.
PDF is available here.
Experimental Neurology (216)2 2009
Abstract
We assessed the capacity of human umbilical cord blood (hUCB)-derived mesenchymal stromal cells (MSCs) to protect and promote regeneration of axotomised neurons within the rat optic system. The optic tract of neonatal rats was transected at the level of the lateral geniculate nucleus, and MSCs were...
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PMID: 19320003
PDF is available here.
PDF is available here.
Abstract
The influence of N-substituents on the mode of reaction of ortho-quinones generated by oxidation of N-substituted dopamine derivatives has been studied. Ortho-quinones with amide, urea or guanidine side chains are relatively stable, with evidence of rearrangement to para-quinomethanes. The N-methylt...
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PMID: 19225678
PDF is available here.
PDF is available here.
Analytical Biochemistry (385)1 2009
Abstract
specificity, linearity (r>0.99), precision (intra and interassay relative standard deviations <5%), robustness, and the limits of detection and quantitation (low and similar for both methods). The main advantage of the use of AUC is to evaluate the antioxidant potential of samples that do not presen...
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PMID: 19027710
PDF is available here.
PDF is available here.
Acta Biochimica Polonica (56)1 2009
Abstract
This work was undertaken to compare cytotoxicity, DNA damaging properties and effect on DNA cleavage by topoisomerase II of the anthracycline drug doxorubicin (DOX) and its two derivatives with a formamidino group containing a cyclic amine moiety such as morpholine (DOXM) or hexamethyleneimine (DOXH...
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PMID: 19238256
PDF is available here.
PDF is available here.
Italian journal of anatomy and embryology = Archivio italiano di anatomia ed embriologia (114)4 2009
Abstract
Our research enables us to describe the organization of the innervation of the lamb retractor penis muscle, highlighting the site of the primary afferent, postganglionic efferent and presumably preganglionic parasympathetic neurons projecting to the muscle....
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PMID: 20578672
PDF is available here.
PDF is available here.
Abstract
A focused library of formamidines having several diversity points has been prepared. The use of isocyanate resin as scavenger may offer several practical advantages over conventional procedures, such as the ease of workup and availability. The technique described herein was performed in a parallel s...
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PMID: 19053503
PDF is available here.
PDF is available here.
Abstract
The influence of Geriforte, an Ayurvedic natural supplement, on the antioxidant defense systems in human erythrocytes and plasma was investigated in an open human clinical study. The ability of Geriforte to inhibit the azo-bis 2-amidinopropane dihydrochloride (AAPH) dependent lysis of erythrocytes w...
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PMID: 20446445
PDF is available here.
PDF is available here.
Renal Failure (31)8 2009
Abstract
Both Melatonin and 1400W were efficient in ameliorating experimental I/R injury of the kidneys. Moreover, melatonin was more effective than 1400W possibly through inhibiting iNOS as well as scavenging free oxygen radicals and peroxynitrite....
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PMID: 19814638
PDF is available here.
PDF is available here.
Abstract
We found that cinnamyl derivative (N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid dihydrochloride (26d, R-142086) with a fluorine atom on the double bond exhibited potent anticoagulant activity and no mutagenic potentia...
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PMID: 19122312
PDF is available here.
PDF is available here.
Abstract
We report that such a situation can be observed in 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH)-treated phosphatidylcholine liposomes in which lipid peroxidation was monitored by oxidation of 4,4-difluoro-5-(4-phenyl-1 3-butadienyl)-4-bora-3a,4a-diaza-s-indacene-3-undecanoic acid (C11-BODIPY...
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PMID: 19323268
PDF is available here.
PDF is available here.
Journal of Neuroscience (28)52 2008
Abstract
We use a transgenic (YFP-H) mouse to demonstrate that cortical layer V projection neurons undergo severe atrophy 4 weeks after thoracic dorsal column injury and that ChABC is neuroprotective for these neurons after ICV infusion. ChABC also prevented cell atrophy after localized delivery to the spina...
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PMID: 19109493
PDF is available here.
PDF is available here.
Abstract
We aimed to develop inhibitors for the human DDAH-1 with improved potency and better relative selectivity for DDAH-1 over NOS. Particularly, the binding pocket of the guanidine-moiety was investigated by screening differently substituted guanidines, amidines and isothioureas in order to collect info...
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PMID: 19013076
PDF is available here.
PDF is available here.
Journal of Organic Chemistry (73)22 2008
Abstract
Our one-pot procedure was successfully applied to the preparation of several compounds of pharmaceutical interest....
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PMID: 18925779
PDF is available here.
PDF is available here.
Abstract
We investigated neuronal number and size in the pars compacta of the pedunculopontine nucleus (PPN) in Parkinson's disease (PD). In PD, the number of Luxol fast blue (LFB) neurons was reduced by 27% from the mean control value (p=0.04) and the cholinergic (choline acetyltransferase, ChAT-positive) n...
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PMID: 18329941
PDF is available here.
PDF is available here.
European Journal of Pharmacology (596)1-3 2008
Abstract
We investigated the effects of several selective CYP omega-hydroxylase inhibitors on myocardial ischemia/reperfusion-induced myocardial apoptosis. Rats were subjected 30 min of ischemia and 2 h of reperfusion. Groups received either 17-octadecynoic acid (17-ODYA, 0.3 or 3 mg/kg), N-methylsulfonyl-12...
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PMID: 18771665
PDF is available here.
PDF is available here.
Abstract
We hypothesized that A2A adenosine receptor (A2A AR) activation causes vasorelaxation through cytochrome P-450 (CYP) epoxygenases and endothelium-derived hyperpolarizing factors, whereas lack of A2A AR activation promotes vasoconstriction through Cyp4a in the mouse aorta. Adenosine 5'-N-ethylcarboxa...
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PMID: 18805895
PDF is available here.
PDF is available here.
Journal of Bacteriology (36)11 2008
Abstract
We report that HET0016 is a noncompetitive inhibitor of rat brain 20-HETE formation, which demonstrates a tissue concentration range for brain inhibition. In addition, we demonstrate that complexation of HET0016 with hydroxypropyl-beta-cyclodextrin results in increased aqueous solubility of HET0016...
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PMID: 18725506
PDF is available here.
PDF is available here.
Abstract
Polycystic kidney diseases are characterized by abnormal proliferation of renal epithelial cells. In this study, the role of 20-hydroxyeicosatetraenoic acid (20-HETE), an endogenous cytochrome P450 metabolite of arachidonic acid with mitogenic properties, was evaluated in cystic renal disease. Daily...
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PMID: 18596124
PDF is available here.
PDF is available here.
Assessment of radical scavenging capacity and lipid peroxidation inhibiting capacity of antioxidant.
Abstract
The role of radical scavenging antioxidants against oxidative stress has received much attention, and the antioxidant capacity has been assessed by various methods. Among them, a method that measures the effect of antioxidant on decay of the probe is one of the most widely used methods. The present...
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PMID: 18717567
PDF is available here.
PDF is available here.
DNA and Cell Biology (27)9 2008
Abstract
We have previously shown that polyamine depletion causes an S phase prolongation, and others have shown that there is an accumulation of Okazaki-like fragments in polyamine-depleted cells. In the present study, we have used the comet assay to investigate polyamine depletion-induced DNA strand breaks...
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PMID: 18554080
PDF is available here.
PDF is available here.
Toxicology In Vitro (22)6 2008
Abstract
We used an in vitro model based on human THP-1 cells to evaluate the inflammatory cytokine/chemokine activation properties of ximelagatran, a drug previously shown to cause elevation of liver transferases in a subset of patients. Treatment of the cells with ximelagatran caused an intracellular accum...
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PMID: 18640260
PDF is available here.
PDF is available here.