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Showing 1-30 of 64 results for "P45907" within Papers
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
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
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
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
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
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
Raza Rasool et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 148, 435-443 (2015-05-09)
New metal polychelates of Mn(II), Co(II), Ni(II), Cu(II) and Zn(II) obtained by the interaction of metal acetates with polymeric Schiff base containing formaldehyde and piperazine, have been investigated. Structural and spectroscopic properties have been evaluated by elemental analysis, FT-IR and
Andrew D Shubin et al.
Tissue engineering. Part A, 21(11-12), 1733-1751 (2015-03-13)
More than 40,000 patients are diagnosed with head and neck cancers annually in the United States with the vast majority receiving radiation therapy. Salivary glands are irreparably damaged by radiation therapy resulting in xerostomia, which severely affects patient quality of
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
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
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
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
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
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
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
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
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
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
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
Carbon dioxide capture with concentrated, aqueous piperazine.
Freeman SA, et al.
International Journal of Greenhouse Gas Control, 4(2), 119-124 (2010)
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
André Brannvoll et al.
Cell reports, 32(1), 107849-107849 (2020-07-09)
Replication-blocking DNA lesions are particularly toxic to proliferating cells because they can lead to chromosome mis-segregation if not repaired prior to mitosis. In this study, we report that ZGRF1 null cells accumulate chromosome aberrations following replication perturbation and show sensitivity
Chang Yoon Moon et al.
Biomaterials, 41, 53-68 (2014-12-20)
Oncolytic adenoviruses (Ads) have shown great promise in cancer gene therapy but their efficacy has been compromised by potent immunological, biochemical, and specific tumor-targeting limitations. To take full advantage of the innate cancer-specific killing potency of oncolytic Ads but also
Luis O'mar Serrano Figueroa et al.
Extremophiles : life under extreme conditions, 19(6), 1183-1192 (2015-10-07)
Soap Lake, located in Washington State, is a naturally occurring saline and alkaline lake. Several organisms inhabiting this lake have been identified as producers of siderophores that are unique in structure. Bacterial isolates, enriched from Soap Lake sediment and water
Patricia Santofimia-Castaño et al.
Toxicology letters, 229(3), 465-473 (2014-07-30)
Ebselen is a seleno-organic compound that causes cell death in several cancer cell types. The mechanisms underlying its deleterious effects have not been fully elucidated. In this study, the effects of ebselen (1 μM-40 μM) on AR42J tumor cells have
John A Christopher et al.
Journal of medicinal chemistry, 56(9), 3446-3455 (2013-03-23)
Biophysical fragment screening of a thermostabilized β1-adrenergic receptor (β1AR) using surface plasmon resonance (SPR) enabled the identification of moderate affinity, high ligand efficiency (LE) arylpiperazine hits 7 and 8. Subsequent hit to lead follow-up confirmed the activity of the chemotype
Paul J Shami et al.
Journal of medicinal chemistry, 49(14), 4356-4366 (2006-07-11)
The literature provides evidence that metabolic nitric oxide (NO) release mediates the cytotoxic activities (against human leukemia and prostate cancer xenografts in mice) of JS-K, a compound of structure R(2)N-N(O)=NO-Ar for which R(2)N is 4-(ethoxycarbonyl)piperazin-1-yl and Ar is 2,4-dinitrophenyl. Here
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