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Girish D Hatnapure et al.
Bioorganic & medicinal chemistry letters, 22(20), 6385-6390 (2012-09-18)
A series of novel 6-methoxy-2-(piperazin-1-yl)-4H-chromen-4-one and 5,7-dimethoxy-2-(piperazin-1-ylmethyl)-4H-chromen-4-one derivatives of biological interest were prepared and screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Among all the compound screened (5a-j and 10k-t), the compounds 5c, 5g
Rongfu Zhang et al.
Biochimica et biophysica acta, 1848(1 Pt B), 329-333 (2014-05-24)
Membrane protein spectroscopic studies are challenging due to the difficulty introduced in preparing homogenous and functional hydrophobic proteins incorporated into a lipid bilayer system. Traditional membrane mimics such as micelles or liposomes have proved to be powerful in solubilizing membrane
Yinghui Mo et al.
Environmental science & technology, 46(24), 13253-13261 (2012-12-05)
Carboxyls are inherent functional groups of thin-film composite polyamide nanofiltration (NF) membranes, which may play a role in membrane performance and fouling. Their surface presence is attributed to incomplete reaction of acyl chloride monomers during the membrane active layer synthesis
Amit K Jha et al.
PloS one, 9(6), e98640-e98640 (2014-06-18)
Osteogenic differentiation of human mesenchymal stem cells (hMSCs) is guided by various physical and biochemical factors. Among these factors, modulus (i.e., rigidiy) of the ECM has gained significant attention as a physical osteoinductive signal that can contribute to endochondral ossification
Jadwiga Handzlik et al.
Bioorganic & medicinal chemistry, 20(14), 4245-4257 (2012-06-29)
The study is focused on a series of 5-arylidenehydantoin derivatives with a phenylpiperazine-hydroxypropyl fragment at N3 of the hydantoin ring. The compounds were assessed on their affinity for α(1)-adrenoceptors and evaluated in functional bioassays for their antagonistic properties. Crystal structures
Jung-Eun Park et al.
Bioorganic & medicinal chemistry letters, 23(6), 1887-1890 (2013-02-12)
To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 2-hydroxy-3-phenoxypropyl piperazine derivatives were synthesized and evaluated for in vitro activities. Compound 6m and 6q showed high selectivity over hERG channel (IC50 ratio of hERG/α1G6m=8.5
Slavka Hamulakova et al.
European journal of medicinal chemistry, 55, 23-31 (2012-07-24)
New tacrine derivatives 5a-d, 6a-d with piperazino-ethyl spacer linked with corresponding secondary amines and tacrine homodimer 8 were synthesized and tested as cholinesterase inhibitors on human acetylcholinesterase (hAChE) and human plasmatic butyrylcholinesterase (hBChE). In most cases the majority of synthesized
Preethi S Nair et al.
PloS one, 9(5), e97337-e97337 (2014-05-23)
Despite increased awareness and diagnostic facilities, 70-80% of the haemophilia A (HA) patients still remain undiagnosed in India. Very little data is available on prevalent mutations in HA from this country. We report fifty mutations in seventy one Indian HA
M K Prashanth et al.
Bioorganic & medicinal chemistry letters, 22(23), 7065-7070 (2012-10-20)
A series of piperamide derivatives (8a-j) was synthesized with various substituted piperidine and piperazine compounds. The prepared compounds were evaluated for antibacterial activity against gram-positive and gram-negative bacteria and antifungal activity by disc diffusion method. The antioxidant activity of the
Enza Lacivita et al.
Journal of medicinal chemistry, 55(14), 6375-6380 (2012-06-29)
Here we report the design, synthesis, and 5-HT(7) receptor affinity of a set of 1-(3-biphenyl)- and 1-(2-biphenyl)piperazines. The effect on 5-HT(7) affinity of various substituents on the second (distal) phenyl ring was analyzed. Several compounds showed 5-HT(7) affinities in the
Liang Li et al.
Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques, 17(4), 447-460 (2015-01-13)
This study investigated influences of concentration and combination of excipients, commonly used in self-emulsifying drug delivery systems (SEDDS), on inhibition of human efflux transporter ABCC2 (MRP2). Ten commonly used excipients of SEDDS with inhibitory effect on MRP2 including Cremophor® EL
Yeon Ah Choi et al.
Biological & pharmaceutical bulletin, 38(2), 208-217 (2015-03-10)
To overcome the low oral bioavailability of morin, a mixed micelle formulation with pharmaceutical excipients that facilitate solubilization and modulate P-glycoprotein (P-gp) was developed and evaluated in vitro and in vivo rats. Morin-loaded mixed micelle formulation with a morin-PluronicF127-Tween80 ratio
Dany Spaggiari et al.
Journal of chromatography. A, 1371, 244-256 (2014-12-03)
The goal of this study was to evaluate the combination of powerful chromatographic methods and compact single quadrupole MS device for simple in vitro cytochrome P450 (CYP) inhibition assay, instead of more expensive triple quadrupole MS/MS detectors. For this purpose
Erik Serrao et al.
Journal of medicinal chemistry, 56(6), 2311-2322 (2013-03-01)
On the basis of an initial molecular modeling study suggesting the favorable binding of the "privileged" fragment 8-hydroxyquinoline with HIV-1 integrase (IN) at the IN-lens epithelium-derived growth factor/p75 (LEDGF/p75) interface , we developed a set of modified 8-hydroxyquinoline fragments demonstrating
Leila Hassanzadeh et al.
Nuclear medicine and biology, 40(2), 227-232 (2012-11-13)
It has been recognized that serotonin plays a main role in various pathological conditions such as anxiety, depression, aggressiveness, schizophrenia, suicidal behavior, panic and autism. 1-(2-Methoxyphenyl) piperazine pharmacophore, a fragment of the true 5-HT(1A) antagonist WAY100635, is found in numerous
P Krishnan et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 102, 379-385 (2012-12-12)
Monohydrate piperazine hydrogen phosphate (MPHP), a semi organic nonlinear optical material has been synthesized and single crystals were grown from aqueous solution by slow evaporation technique. Single crystal X-ray diffraction study on grown crystal reveals that they belong to monoclinic
Abbas Ahmadi et al.
Mini reviews in medicinal chemistry, 12(12), 1282-1292 (2012-08-11)
In addition to their antihistamine effects, H1-receptor antagonists possess pharmacological properties that are not uniformly distributed among this class of drugs, such as anti-inflammatory, anti-allergic and antiplatelet activities. In this paper, Cyclizine (1-benzhydryl-4-methyl-piperazine, I), bromodiphenhydramine (2-[(4-bromophenyl)-phenylmethoxy]-N, N-dimethylethanamine, II) and some
Rajangam Vinodh et al.
Journal of nanoscience and nanotechnology, 14(6), 4639-4648 (2014-04-18)
Chloro-functionalized mesoporous MCM-41, SBA-15, MCM-48 and KIT-6 were synthesized by co-condensation of 3-chloropropyl-trimethoxy-silane (CPTMS) and rice husk ash sodium silicate solution, which is subsequently grafted with a heterocyclic amine, homopiperazine (HPZ). X-ray powder diffraction and BET analysis of the chloro-functionalized
Kasper Kristensen et al.
Biochimica et biophysica acta, 1838(12), 2994-3002 (2014-08-20)
Fluorescence correlation spectroscopy (FCS) is a powerful experimental technique that in recent years has found numerous applications for studying biological phenomena. In this article, we scrutinize one of these applications, namely, FCS as a technique for studying leakage of fluorescent
Raman Sharma et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(11), 2143-2161 (2012-08-17)
The disposition of 3,3-difluoropyrrolidin-1-yl{(2S,4S)-4-[4-(pyrimidin-2-yl)piperazin-1-yl]pyrrolidin-2-yl}methanone (PF-00734200), a dipeptidyl peptidase IV inhibitor that progressed to phase 3 for the treatment of type 2 diabetes, was examined in rats, dogs, and humans after oral administration of a single dose of [(14)C]PF-00734200. Mean recoveries
Shu Cai et al.
Bioresource technology, 130, 536-542 (2013-01-22)
Piperazine is widely used as an intermediate in the manufacture of insecticides, rubber chemicals, corrosion inhibitors, and urethane. In this study, a highly effective piperazine-degrading bacteria strain, TOH, was isolated from the acclimated activated sludge of a pharmaceutical plant. This
Kais Kasem et al.
Experimental and molecular pathology, 97(1), 99-104 (2014-06-15)
JK1 is a novel cancer-related gene with unknown functional role in carcinogenesis. The aim of this study is to investigate the role of JK1 gene in carcinogenesis in an in vitro cell proliferation and migration analysis model. Small hairpin RNAs
Amy H Van Hove et al.
Biomaterials, 35(36), 9719-9730 (2014-09-03)
Despite the recent expansion of peptide drugs, delivery remains a challenge due to poor localization and rapid clearance. Therefore, a hydrogel-based platform technology was developed to control and sustain peptide drug release via matrix metalloproteinase (MMP) activity. Specifically, hydrogels were
Janie Sheridan et al.
Drug and alcohol review, 26(3), 335-343 (2007-04-25)
In this Harm Reduction Digest Sheridan, Butler, Wilkins and Russell address the emergent phenomenon of so-called 'legal party pills' which have become a significant drug issue in New Zealand and elsewhere. Although banned in a number of countries, they are
G L Silva et al.
Journal of chromatography. A, 1352, 46-54 (2014-06-14)
An investigation of the adsorption mechanism of lysozyme onto carboxymethyl cellulose (CMC) was conducted using flow calorimetry and adsorption isotherm measurements. This study was undertaken to provide additional insight into the underlying mechanisms involved in protein adsorption that traditional approaches
Martine Keenan et al.
Bioorganic & medicinal chemistry, 21(7), 1756-1763 (2013-03-07)
A scaffold hopping exercise undertaken to expand the structural diversity of the fenarimol series of anti-Trypanosoma cruzi (T. cruzi) compounds led to preparation of simple 1-[phenyl(pyridin-3-yl)methyl]piperazinyl analogues of fenarimol which were investigated for their ability to inhibit T. cruzi in
Carl Cheadle et al.
Dalton transactions (Cambridge, England : 2003), 42(14), 4931-4946 (2013-02-07)
A new multidentate bifunctional organic ligand – di-N,N′-(2-cyano-2-oximinoacetyl)piperazine – was synthesized in high yield using a two-step procedure carried out under ambient conditions. At first, the reaction of piperazine and neat methylcyanoacetate led to the di-N,N′-(cyanoacetyl)piperazine (1), which then was
Marilena Gregorini et al.
BMC immunology, 15, 44-44 (2014-10-04)
In former studies we showed in a rat model of renal transplantation that Mesenchymal Stromal Cells (MSC) prevent acute rejection in an independent way of their endowing in the graft. In this study we investigated whether MSC operate by resetting
Rahul V Patel et al.
Mini reviews in medicinal chemistry, 13(11), 1579-1601 (2013-07-31)
This article purposes to provide insights to piperazine based molecular designs that will facilitate drug discovery program in future. In our pursuit to summarize the reservoir of bioactive agents, and in line with the synthetic economy of new heterocycles, many
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
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