Pyrimidinones are heterocyclic organic compounds that consist of a pyrimidine ring fused with a ketone group, which have significant applications in medicinal chemistry due to their wide range of biological activities, including antibacterial, antiviral, and anticancer properties.

Relationships between phosphatidic acid and cyclic nucleotide phosphodiesterases in activated human blood mononuclear cells. (1/851)

We have previously shown that mitogenic activation of human PBMC rapidly increases both the intracellular phosphatidic acid (PA) level and cyclic nucleotide phosphodiesterase (PDE) activity, with time-course responses, suggesting a causative relationship between the two events. PA also directly stimulated cAMP-PDE activity in acellular systems. Thus the mitogenic properties of PA night be due to its ability to lower the level of cAMP, a negative effector of lymphocyte activation, through PDE activation. In this study, human PBMC were stimulated either with the mitogenic lectin ConA, the anti-CD3 mAb OKT3, or the phorbol ester TPA. All three agonists increased the radiolabeled PA level and the PA mass in treated cells and simultaneously increased cytosolic and particulate cAMP- and cGMP-PDE activities, with significant positive correlations between PA accumulation and PDE activities. Furthermore, the ConA-induced PDE activation was dose-dependently reduced by treatment of PBMC with the diacylglycerol-kinase inhibitor R59022. This compound also dose-dependently lowered the PA level and inhibited the proliferative response to ConA. In addition, TPA-induced PDE activation was totally abolished by ethanol, which strongly reduced PA accumulation in response to the phorbol ester. These data suggest that PA increase may be linked to mitogen-induced PDE activation. Experiments performed in the presence of rolipram indicated that ConA and TPA stimulated both the rolipram-sensitive PDE4 and the rolipram-insensitive PDE activities, OKT3 being more active on PDE4. All three agonists stimulated the cGMP-specific PDE5. These results suggest that PA is an important component of the mechanisms that maintain a low level of cyclic nucleotides, which is a prerequisite for an optimal lymphoproliferative response.  (+info)

Novel derivatives of phenethyl-5-bromopyridylthiourea and dihydroalkoxybenzyloxopyrimidine are dual-function spermicides with potent anti-human immunodeficiency virus activity. (2/851)

Sexually active women represent the fastest growing HIV/AIDS (human immunodeficiency virus/acquired immunodeficiency syndrome) risk group. In an effort to develop a vaginal microbicidal contraceptive potentially capable of preventing HIV transmission as well as providing fertility control, we have synthesized novel non-nucleoside inhibitors (NNIs) of HIV-1 reverse transcriptase (RT) and examined them for dual-function anti-HIV and spermicidal activity. Structure-based drug design by use of a computer docking procedure for the NNI binding pocket generated from nine RT-NNI crystal structures led to the synthesis of three novel NNIs: N-[2-(2, 5-dimethoxyphenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (D-PBT); N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (F-PBT); and 5-isopropyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-on e (S-DABO). The anti-HIV activity of these NNIs was compared with that of trovirdine and virucidal/spermicide, nonoxynol-9 (N-9), by measuring viral RT activity and p24 antigen production as markers of viral replication using HTLVIIIB-infected human peripheral blood mononuclear cells (PBMCs). The effects on sperm motion kinematics and sperm membrane integrity were examined by computer-assisted sperm analysis and by confocal laser scanning microscopy (CLSM), respectively. The growth-inhibitory effects of NNI versus N-9 against normal human ectocervical and endocervical epithelial cells were tested using the MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) assay. All three NNIs were potent inhibitors of purified recombinant HIV RT and abrogated HIV replication in PBMCs at nanomolar concentrations (IC50 < 1 nM) when compared with N-9 or trovirdine (IC50 values of 2.2 microM and 0.007 microM, respectively). Two NNIs, F-PBT and S-DABO, also exhibited concentration- and time-dependent spermicidal activity. The drug concentration required to inhibit sperm motility by 50% (EC50 values) for the lead compound F-PBT versus N-9 was 147 microM and 81 microM, respectively. Sperm-immobilizing activity induced by F-PBT and S-DABO was rapid (t1/2 = 7-13 min) and irreversible. Unlike that of N-9, spermicidal activity of F-PBT and S-DABO was not accompanied by loss of acrosomal membrane as detected by fluorescent-lectin binding assay and CLSM. Whereas N-9 was cytotoxic to normal human ectocervical and endocervical cells at spermicidal doses, both F-PBT and S-DABO were selectively spermicidal. We conclude that as potent anti-HIV agents with spermicidal activity and reduced cytotoxicity, F-PBT and S-DABO show unique clinical potential to become the active ingredients of a vaginal contraceptive for women who are at high risk for acquiring HIV by heterosexual vaginal transmission.  (+info)

Purified photoproducts of merocyanine 540 trigger cytochrome C release and caspase 8-dependent apoptosis in human leukemia and melanoma cells. (3/851)

If the interplay between caspase proteases and mitochondria decide the fate of the cell during apoptosis, they may constitute useful molecular targets for novel drug design. We have shown that photoactivated merocyanine 540 (pMC540) triggers caspase-mediated apoptosis in HL60 leukemia and M14 melanoma cells. Because pMC540 is a mixture of photoproducts, we set out to purify the biologically active component(s) from this mixture and to investigate their ability to directly activate intracellular caspases and/or trigger mitochondrial events associated with apoptosis. Two photoproducts, namely C1 and C2, purified and characterized by mass spectroscopy and nuclear magnetic resonance (NMR) analysis, effectively induced apoptosis in HL60 and M14 cells. Interestingly, both C1 and C2 induced non-receptor-dependent activation of caspase 8, which was responsible for the downstream activation of caspase 3 and cell death. Both compounds induced the release of cytochrome C from mitochondria of tumor cells and from purified rat liver mitochondria; however, different mechanisms were operative in cytochrome C translocation in response to C1 or C2. C1-induced cytochrome C release was mediated by the mitochondrial permeability transition (MPT) pore and accompanied by a decrease in mitochondrial transmembrane potential (triangle uppsim), whereas cytochrome C release in response to C2 was independent of MPT pore opening. These findings do not exclude the possibility that changes in mitochondrial triangle uppsim are critical for apoptosis in some instances, but support the notion that this may not be a universal step in the apoptotic process. Thus, identification of two novel anticancer agents that directly activate effector components of the apoptotic pathway could have potential implications for the development of newer chemotherapeutic drugs.  (+info)

Potent inhibition of the cytochrome P-450 3A-mediated human liver microsomal metabolism of a novel HIV protease inhibitor by ritonavir: A positive drug-drug interaction. (4/851)

ABT-378 is a potent in vitro inhibitor of the HIV protease and is currently being developed for coadministration with another HIV protease inhibitor, ritonavir, as an oral therapeutic treatment for HIV infection. In the present study, the effect of ritonavir, a potent inhibitor of cytochrome P-450 (CYP) 3A, on the in vitro metabolism of ABT-378 was examined. Furthermore, the effect of ABT-378-ritonavir combinations on several CYP-dependent monooxygenase activities in human liver microsomes was also examined. ABT-378 was found to undergo NADPH- and CYP3A4/5-dependent metabolism to three major metabolites, M-1 (4-oxo) and M-3/M-4 (4-hydroxy epimers), as well as several minor oxidative metabolites in human liver microsomes. The mean apparent K(m) and V(max) values for the metabolism of ABT-378 by human liver microsomes were 6.8 +/- 3.6 microM and 9.4 +/- 5.5 nmol of ABT-378 metabolized/mg protein/min, respectively. Ritonavir inhibited human liver microsomal metabolism of ABT-378 potently (K(i) = 0.013 microM). The combination of ABT-378 and ritonavir was much weaker in inhibiting CYP-mediated biotransformations than ritonavir alone, and the inhibitory effect appears to be primarily due to the ritonavir component of the combination. The ABT-378-ritonavir combinations (at 3:1 and 29:1 ratios) inhibited CYP3A (IC(50) = 1.1 and 4.6 microM), albeit less potently than ritonavir (IC(50) = 0.14 microM). Metabolic reactions mediated by CYP1A2, CYP2A6, and CYP2E1 were not affected by the ABT-378-ritonavir combinations. The inhibitory effects of ABT-378-ritonavir combinations on CYP2B6 (IC(50) = >30 microM), CYP2C9 (IC(50) = 13.7 and 23.0 microM), CYP2C19 (IC(50) = 28.7 and 38.0 microM), and CYP2D6 (IC(50) = 13.5 and 29.0 microM) were marginal and are not likely to produce clinically significant drug-drug interactions.  (+info)

Tissue factor activity is increased in human endothelial cells cultured under elevated static pressure. (5/851)

We tested the hypothesis that elevated blood pressure, a known stimulus for vascular remodeling and an independent risk factor for the development of atherosclerotic disease, can modulate basal and cytokine-induced tissue factor (TF; CD 142) expression in cultured human endothelial cells (EC). Using a chromogenic enzymatic assay, we measured basal and tumor necrosis factor-alpha (TNF-alpha; 10 ng/ml, 5 h)-induced TF activities in human aortic EC (HAEC) and vena cava EC (HVCEC) cultured at atmospheric pressure and at 170 mmHg imposed pressure for up to 48 h. Basal TF activities were 22 +/- 10 U/mg protein for HAEC and 14 +/- 9 U/mg protein for HVCEC and were upregulated in both cell types >10-fold by TNF-alpha. Exposure to pressure for 5 h induced additional elevation of basal TF activity by 47 +/- 16% (P < 0.05, n = 6) for HAEC and 17 +/- 5% (P < 0.05, n = 3) for HVCEC. Pressurization also enhanced TF activity in TNF-alpha-treated cells from 240 +/- 28 to 319 +/- 32 U/mg protein in HAEC (P < 0.05, n = 4) and from 148 +/- 25 to 179 +/- 0.8 U/mg protein (P < 0.05, n = 3) in HVCEC. Cytokine stimulation caused an approximately 100-fold increase in steady-state TF mRNA levels in HAEC, whereas pressurization did not alter either TF mRNA or cell surface antigen expression, as determined by quantitative RT-PCR methodology and ELISA. Elevated pressure, however, modulated the EC plasma membrane organization and/or permeability as inferred from the increased cellular uptake of the fluorescent amphipathic dye merocyanine 540 (33 +/- 7%, P < 0.05). Our data suggest that elevated static pressure modulates the hemostatic potential of vascular cells by modifying the molecular organization of the plasma membrane.  (+info)

A protein kinase C-beta-selective inhibitor ameliorates neural dysfunction in streptozotocin-induced diabetic rats. (6/851)

Increased protein kinase C (PKC) activity has been implicated in the pathogenesis of diabetic retinopathy and nephropathy. However, the role of PKC in diabetic neuropathy remains unclear. The present study was conducted to compare the effect of PKC inhibition by a PKC-beta-selective inhibitor, LY333531 (LY), on diabetic nerve dysfunction with that of an aldose reductase inhibitor, NZ-314 (NZ). Streptozotocin-induced diabetic rats were treated with or without LY and/or NZ for 4 weeks, and motor nerve conduction velocity (MNCV), coefficient of variation of R-R interval (CVR-R), sciatic nerve blood flow (SNBF), peak latencies of oscillatory potentials on electroretinogram, PKC activities in membranous and cytosolic fractions of sciatic nerves, and polyol contents in the tail nerves were measured. Untreated diabetic rats demonstrated delayed MNCV, decreased CVR-R, reduced SNBF, and prolonged peak latencies of oscillatory potentials. Treatment with LY as well as NZ prevented all these deficits in diabetic rats. There were no significant differences in PKC activities in membranous or cytosolic fractions of sciatic nerves between normal and diabetic rats. Treatment with neither LY nor NZ altered PKC activities. Nerve myo-inositol depletion in diabetic rats was ameliorated not only by NZ, but also by LY. These observations suggest that inhibition of PKC-beta by LY may have a beneficial effect in preventing the development of diabetic nerve dysfunction, and that this effect may be mediated through its action on the endoneurial micro-vasculature.  (+info)

Lipid composition determines the effects of arbutin on the stability of membranes. (7/851)

Arbutin (hydroquinone-beta-D-glucopyranoside) is an abundant solute in the leaves of many freezing- or desiccation-tolerant plants. Its physiological role in plants, however, is not known. Here we show that arbutin protects isolated spinach (Spinacia oleracea L.) thylakoid membranes from freeze-thaw damage. During freezing of liposomes, the presence of only 20 mM arbutin led to complete leakage of a soluble marker from egg PC (EPC) liposomes. When the nonbilayer-forming chloroplast lipid monogalactosyldiacylglycerol (MGDG) was included in the membranes, this leakage was prevented. Inclusion of more than 15% MGDG into the membranes led to a strong destabilization of liposomes during freezing. Under these conditions arbutin became a cryoprotectant, as only 5 mM arbutin reduced leakage from 75% to 20%. The nonbilayer lipid egg phosphatidylethanolamine (EPE) had an effect similar to that of MGDG, but was much less effective, even at concentrations up to 80% in EPC membranes. Arbutin-induced leakage during freezing was accompanied by massive bilayer fusion in EPC and EPC/EPE membranes. Twenty percent MGDG in EPC bilayers completely inhibited the fusogenic effect of arbutin. The membrane surface probes merocyanine 540 and 2-(6-(7-nitrobenz-2-oxa-1, 3-diazol-4-yl)amino)hexanoyl-1-hexadecanoyl-sn-glycero-3-phosph ocholi ne (NBD-C(6)-HPC) revealed that arbutin reduced the ability of both probes to partition into the membranes. Steady-state anisotropy measurements with probes that localize at different positions in the membranes showed that headgroup mobility was increased in the presence of arbutin, whereas the mobility of the fatty acyl chains close to the glycerol backbone was reduced. This reduction, however, was not seen in membranes containing 20% MGDG. The effect of arbutin on lipid order was limited to the interfacial region of the membranes and was not evident in the hydrophobic core region. From these data we were able to derive a physical model of the perturbing or nonperturbing interactions of arbutin with lipid bilayers.  (+info)

Extensive electroporation abolishes experimentally induced shape transformations of erythrocytes: a consequence of phospholipid symmetrization? (8/851)

As shown in earlier work (M.M. Henszen et al., Mol. Membr. Biol. 14 (1997) 195-204), exposure of erythrocytes to single brief electric field pulses (5-7 kV cm(-1)) enhances the transbilayer mobility of phospholipids and produces echinocytes which can subsequently be transformed into stomatocytes in an ATP-dependent process. These shape transformations arise from partly reversible changes of the transbilayer disposition of phospholipids, in agreement with the bilayer couple concept. Extensive membrane modification by repetitive (+info)

Pyrimidinones are a class of heterocyclic organic compounds that contain a pyrimidine ring fused with a ketone group. The basic structure of a pyrimidinone consists of two nitrogen atoms and four carbon atoms in a six-membered ring, with a carbonyl (C=O) group attached to one of the carbon atoms.

In a medical context, pyrimidinones are important because many naturally occurring and synthetic compounds that contain this structure have been found to have biological activity. For example, some pyrimidinones have antiviral, antibacterial, or anticancer properties, making them useful in the development of new drugs for various medical conditions.

One well-known drug that contains a pyrimidinone ring is the antiviral medication Ribavirin, which is used to treat hepatitis C and certain viral hemorrhagic fevers. Other pyrimidinones are being studied for their potential therapeutic benefits in areas such as cancer therapy, neuroprotection, and inflammation.

2,5-diamino-6-(ribosylamino)-4(3H)-pyrimidinone+5'-phosphate+reductase at the U.S. National Library of Medicine Medical Subject ... 2,5-diamino-6-(ribosylamino)-4(3H)-pyrimidinone 5'-phosphate reductase (EC 1.1.1.302, 2,5-diamino-6-ribosylamino-4(3H)- ... pyrimidinone 5'-phosphate reductase, MjaRED, MJ0671 (gene)) is an enzyme with systematic name 2,5-diamino-6-(5-phospho-D- ... pyrimidinone 5'-phosphate reductase of Methanocaldococcus jannaschii". Journal of Molecular Biology. 359 (5): 1334-51. doi: ...
Skulnick HI, Weed SD, Eidson EE, Renis HE, Wierenga W, Stringfellow DA (December 1985). "Pyrimidinones. 1. 2-Amino-5-halo-6- ... aryl-4(3H)-pyrimidinones. Interferon-inducing antiviral agents". Journal of Medicinal Chemistry. 28 (12): 1864-9. doi:10.1021/ ...
A third type of lesion is a Dewar pyrimidinone, formed by a reversible isomerization of the 6-4 photoproduct upon further ... A 6-4 photoproduct (6-4 pyrimidine-pyrimidone or 6-4 pyrimidine-pyrimidinone) is an alternate dimer consisting of a single ... ISBN 978-0-8053-5015-9.[pages needed] Taylor JS, Cohrs M (1987). "DNA, light and Dewar pyrimidinones: the structure and ...
... and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5". J Med Chem. 55 (23): 10540-10550. doi: ...
Sweet, F.; Fissekis, J. D. (1973). "Synthesis of 3,4-dihydro-2(1H)-pyrimidinones and the mechanism of the Biginelli reaction". ...
"Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ". Bioorganic & Medicinal ...
"Synthesis of Fused Pyrimidinone and Quinolone Derivatives in an Automated High-Temperature and High-Pressure Flow Reactor". ...
Reaction of the former with amidines to give 2-substituted pyrimidines, with urea to give 2-pyrimidinones, and guanidines to ...
Another condensation can happen with 2,5,6-triamino-4(3H)pyrimidinone giving 6-acetyl-2-amino-7-methyl-4(3H)pteridinone. ...
... and pyrimidinones". Journal of the American Chemical Society. 124 (39): 11689-11698. doi:10.1021/ja0271375. PMID 12296735. ...
A two-year study was conducted in the dog who was given a diet containing phenylurea and pyrimidinone at daily doses of 0 + 0; ... pyrimidinone mixture. No other effects due to treatment have been reported. The NOEL was 180 + 60 mg/kg. A 2-year study was ... pyrimidinone mixture at the daily doses, in mg/kg of body weight of 0 + 0; 50 + 17; 150 + 50; 300 + 100. At the highest dosage ... pyrimidinone also called 4,4'-dinitrocarbanilide (DNC) and 2-hydroxy - 4,6 dimethylpyrimidine (HDP). The DNC represents the ...
... pyrimidinones MeSH D03.383.742.698.122 - alloxan MeSH D03.383.742.698.253 - barbiturates MeSH D03.383.742.698.253.077 - ...
Anderson, J. C.; Smith, S. C. (1990). "Oxodiperoxymolybdenum(pyridine)-1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone (MoO5 ...
... pyrimidinone and 3-amino-1,2,4-triazole derivatives". Bioorganic & Medicinal Chemistry. 23 (3): 480-7. doi:10.1016/j.bmc. ...
Application to the Synthesis of a Novel Pyrimidinone Building Block", Synthetic Communications (in German), vol. 34, no. 5, pp ...
... pyrimidinone, 5-amino-1,4-dihydro- 7H-v-Triazolo(4,5-d)pyrimidin-7-one, 5-amino-1,6-dihydro- 8 AG 8azaG Azaguanine Azaguanine-8 ...
... pyrimidinone 5′-phosphate reductase EC 1.1.1.303: diacetyl reductase [(R)-acetoin forming] EC 1.1.1.304: diacetyl reductase [(S ...
... pyrimidinone) in good yields was reported in 2001. These products were obtained by heating formamide in the presence of simple ...
2,5-diamino-6-(ribosylamino)-4(3H)-pyrimidinone+5-phosphate+reductase at the U.S. National Library of Medicine Medical Subject ... 2,5-diamino-6-(ribosylamino)-4(3H)-pyrimidinone 5-phosphate reductase (EC 1.1.1.302, 2,5-diamino-6-ribosylamino-4(3H)- ... pyrimidinone 5-phosphate reductase, MjaRED, MJ0671 (gene)) is an enzyme with systematic name 2,5-diamino-6-(5-phospho-D- ... pyrimidinone 5-phosphate reductase of Methanocaldococcus jannaschii". Journal of Molecular Biology. 359 (5): 1334-51. doi: ...
4(1H)-Pyrimidinone,. 5-(carboxymethyl)-. 2,3-dihydro-1-β-D-r. ibofuranosyl-2-thio. xo- [ACD/Index Name] ... 4(1H)-pyrimidinone *Molecular FormulaC11H14N2O7S ...
... pyrimidinone, 2-Ethoxy-5-fluoro-4(3H)-pyrimidinone, 5-Flucytosine, Piperonal and Floramelon as main products. ... pyrimidinone(cas:1480-96-2)--Suqian Wanhetai Chemical Co., Ltd. ...
Pyrimidinone, 4-amino-5-fluoro-1-[(2S,5R)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-. CAS 137530-41-7. MDL Number:MFCD00870858. ... 137530-41-7 , 2(1H)-Pyrimidinone, 4-amino-5-fluoro-1-[(2S,5R)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-. CAS No: 137530-41-7 ... 2(1H)-Pyrimidinone, 4-amino-5-fluoro-1-[(2S,5R)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]- ...
Categories: Pyrimidinones Image Types: Photo, Illustrations, Video, Color, Black&White, PublicDomain, CopyrightRestricted 6 ...
2(1H)-Pyrimidinone,. 4-amino-1-(5-O-pho. sphono-β-L-ribofura. nosyl)- [ACD/Index Name] ...
Synthesis and molecular modelling studies of pyrimidinones and pyrrolo[3,4-d]-pyrimidinodiones as new antiplasmodial compounds ...
Molecular Docking and Biophysical Studies for Antiproliferative Assessment of Synthetic Pyrazolo-Pyrimidinones Tethered with ...
1,3-Dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone ...
... pyrimidinone, 6-amino- , ,JCHEM_VEBER_RULE, 0 $$$$ ...
Chemical Name: 2-(Hexylthio)-6-hydroxy-4(3H)-pyrimidinone Purity: ≥98% (HPLC) ...
5-Nitro-4(1H)-Pyrimidinone 3749-47-1. Inquire. 2,3-Dimethylbiphenyl 3864-18-4. Inquire. ...
2-[(4-methoxybenzyl)sulfanyl]-6-methyl-4(3H)-pyrimidinone. 63384-61-2. ...
Complex-forming properties of synthetic pyrimidinone nucleosides with Ag(I) ions in an aqueous solution. Marek Pająk, Magdalena ...
CAS Name: 4-Amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone ...
Chemical Name: 2,3-Dihydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-pyrimidinone ...
Hannah, Duncan Robert (1997) The chemistry of imidazoles and pyrimidinones. PhD thesis, University of Nottingham. ...
Lu 201640; 2-[[3-[4-[2-(1,1-Dimethylethyl)-6-(trifluoromethyl)-4-pyrimidinyl]-1-piperazinyl]propyl]thio]-4(3H)-pyrimidinone; 2 ... 3-[4-[2-(1,1-Dimethylethyl)-6-(trifluoromethyl)-4-pyrimidinyl]-1-piperazinyl]propyl]thio]-4(1H)-pyrimidinone. ...
6-amino-5-fluoro-2(1H)-pyrimidinone. IUPAC Name. 4-Amino-5-fluoro-2(1H)-pyrimidinone ...
5-iodo-2-pyrimidinone-2′-deoxyribose (IPdR), in HCT116 MMR− s.c. xenografts compared with HCT116 MMR+ s.c. xenografts (30). In ... deficient human colon cancer xenografts with 5-iodo-2-pyrimidinone-2-deoxyribose. Clin Cancer Res ...
Synonyms: CTK3G0733, CTK3G0742, CTK8I1313, 4(3H)-Pyrimidinone, 2-(2-hydroxyethenyl)-, Acetaldehyde, 2-(3,4-dihydro-4-oxo-2(1H)- ...
Pyrimidinones/economics, Ritonavir/economics, Substance Abuse, Intravenous, Time Factors, Treatment Outcome, Unsafe Sex, ...
Part 2: Pyridone- and pyrimidinone-derived systems. Two screening campaigns using commercial (Chembridge DiverSET) and ... proprietary (Chemical Biology Consortium Sweden, CBCS) compound libraries, revealed a number of pyridone- and pyrimidinone- ...
Abstract: The present invention relates to new pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 activity, ...
Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such ... Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such ... Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such ...
Preparation of analogues of cytosine and 2-pyrimidinone nucleosides and their effect on bacterial (Escherichia coli A 19) ... 2,3-Dideoxy- and 3-Azido-2,3-dideoxynucleosides of 5-Phenyl-2(1H)-pyrimidinone. Preparation of 2,3-Dideoxypentofuranoses ... Synthesis of 5-Phenyl-2(1H)-pyrimidinone Nucleosides. 1996, Vol. 61, Issue 3, pp. 458-477 [Abstract] ...
Mechanism and mode of action of 5-iodo-2-pyrimidinone 2-deoxyribonucleoside, a potent anti-herpes simplex virus compound, in ... Mechanism and mode of action of 5-iodo-2-pyrimidinone 2-deoxyribonucleoside, a potent anti-herpes simplex virus compound, in ...
  • The latter virtual screening hit, a pyrimidinone derivative VS-8‎ was synthesized and the structure was modified by substitution in positions 2, 4, 5 and 6 of the pyrimidine ring. (uni-wuerzburg.de)
  • Here, we show a proof-of-concept study in which a supramolecular approach based on ureido-pyrimidinone (UPy) was used, which allows for modular functionalization. (mdrresearch.nl)
  • The convenient control of the complex stability renders these systems highly suitable for the construction of more complex, directionally defined surface-immobilized supramolecular architectures, as well as for the study of pyrimidinone-based supramolecular polymers at surfaces using AFM approaches. (mtpgroup.nl)
  • Stamina-Rx utilizes xanthoparmelia scabrosa, a natural source of Pyrazolo pyrimidinone (a core component of leading prescription medications for impotence). (illpumpyouup.com)
  • Force-extension curves measured between pyrimidinone derivatives in hexadecane (dimer interaction). (mtpgroup.nl)
  • We identified the trifluoromethyl pyrimidinone series of compounds in a whole-cell screen against Mycobacterium tuberculosis . (nih.gov)
  • The researchers prepared a chemical soup made from a host of ingredients: aryl iodide and alkyl iodide substrates, an NiI 2 catalyst, bipyridine and bis(diphenylphosphino)-benzene ligands, a pyridine additive, manganese powder as a reducing agent, and a pyrimidinone solvent (DMPU). (acs.org)
  • The complex formation of 2-ureido-4[1H]-pyrimidinone moieties at Au surfaces through quadruple hydrogen bonds can be conveniently controlled via solvent or temperature. (mtpgroup.nl)
  • For this purpose 2-ureido-4[1H]-pyrimidinone moieties at gold (Au) surfaces were studied (Figure 5). (mtpgroup.nl)
  • Although substituted pyrimidinones and guanosines were not able to induce new DNA synthesis or antibody production in small B cells, both classes of compounds increased the expression of Ia antigens on the surface of both small and large B cells. (ox.ac.uk)
  • These data, together with the recent observations that 8-BrGuo, like ABPP and AIPP, can stimulate NK and cytotoxic macrophage activity via the induction of interferon, strongly suggest that 5-halo-6-phenyl pyrimidinones and 8-substituted guanosines belong to the same structural class of biological response modifiers. (ox.ac.uk)
  • An overview of Genetic Toxicology Bacterial Mutagenicity study conclusions related to 6-Hydroxy-4(1H)-pyrimidinone (1193-24-4). (nih.gov)