P45907

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Degradation of piperazine by Paracoccus sp. TOH isolated from activated sludge.

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

Quantification of leakage from large unilamellar lipid vesicles by fluorescence correlation spectroscopy.

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

Homopiperazine grafted mesoporous silicas from rice husk ash for CO2 adsorption.

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

Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human.

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

Carbon dioxide capture with concentrated, aqueous piperazine.

Freeman SA, et al.

International Journal of Greenhouse Gas Control, 4(2), 119-124 (2010)

Synthesis and anti-inflammatory effects of new piperazine and ethanolamine derivatives of H(1)-antihistaminic drugs.

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

Growth, nonlinear optical, thermal, dielectric and laser damage threshold studies of semiorganic crystal: monohydrate piperazine hydrogen phosphate.

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

Synthesis, radiolabeling and bioevaluation of a novel arylpiperazine derivative containing triazole as a 5-HT1A receptor imaging agents.

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

Comparison of liquid chromatography and supercritical fluid chromatography coupled to compact single quadrupole mass spectrometer for targeted in vitro metabolism assay.

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

Fragment-based discovery of 8-hydroxyquinoline inhibitors of the HIV-1 integrase-lens epithelium-derived growth factor/p75 (IN-LEDGF/p75) interaction.

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

Mutations in intron 1 and intron 22 inversion negative haemophilia A patients from Western India.

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

Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers.

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

Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.

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

Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent.

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

Characterizing the structure of lipodisq nanoparticles for membrane protein spectroscopic studies.

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

Synthesis, characterization, antidepressant and antioxidant activity of novel piperamides bearing piperidine and piperazine analogues.

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

Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.

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

Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with α₁-adrenoceptor antagonistic properties.

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

Inhibition of human efflux transporter ABCC2 (MRP2) by self-emulsifying drug delivery system: influences of concentration and combination of excipients.

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

Biologically active and thermally stable polymeric Schiff base and its metal polychelates: Their synthesis and spectral aspects.

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

Development of poly(ethylene glycol) hydrogels for salivary gland tissue engineering applications.

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

Enhanced oral bioavailability of morin administered in mixed micelle formulation with PluronicF127 and Tween80 in rats.

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

Controlling osteogenic stem cell differentiation via soft bioinspired hydrogels.

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

Improved antifouling properties of polyamide nanofiltration membranes by reducing the density of surface carboxyl groups.

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

Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.

Mitsunori Kono et al.

Bioorganic & medicinal chemistry, 21(1), 28-41 (2012-12-12)

A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the lead compound 3

Ivermectin and piperazine toxicoses in dogs and cats.

R A Lovell

The Veterinary clinics of North America. Small animal practice, 20(2), 453-468 (1990-03-01)

Review of all reports involving anthelmintics in dogs and cats to the IAPIC between January 1, 1986 and August 10, 1988, revealed that ivermectin (extra-label use) and piperazine accounted for over 50% of the calls assessed as toxicoses and suspected

Improved solvent formulations for efficient CO₂ absorption and low-temperature desorption.

Francesco Barzagli et al.

ChemSusChem, 5(9), 1724-1731 (2012-07-11)

This experimental study describes efficient CO₂ capture by 2-amino-2-methyl-1-propanol (AMP)/piperazine (PZ) in ethylene glycol monoethyl ether (EGMEE, 2-ethoxyethanol) containing approximately 15 wt % of water. In these experiments, the solvent is continuously circulated between the absorber (packed-bed reactor at 30, 40

Design and optimization of novel (2S,4S,5S)-5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxy-2-isopropylhexanamides as renin inhibitors.

Yuji Nakamura et al.

Bioorganic & medicinal chemistry letters, 22(14), 4561-4566 (2012-06-26)

Introduction of the 2,2-dimethyl-4-phenylpiperazin-5-one scaffold into the P(3)-P(1) portion of the (2S,4S,5S)-5-amino-6-dialkylamino-4-hydroxy-2-isopropylhexanamide backbone dramatically increased the renin inhibitory activity without using the interaction to the S(3)(sp) pocket. Compound 31 exhibited >10,000-fold selectivity over other human proteases, and 18.5% oral bioavailability

Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone.

Natalia Szkaradek et al.

Bioorganic & medicinal chemistry, 21(2), 514-522 (2012-12-19)

A series of 9 piperazine derivatives of xanthone were synthesized and evaluated for cardiovascular activity. The following pharmacological experiments were conducted: the binding affinity for adrenoceptors, the influence on the normal electrocardiogram, the effect on the arterial blood pressure and

The seleno-organic compound ebselen impairs mitochondrial physiology and induces cell death in AR42J cells.

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

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