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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
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
Hideto Fujiwara et al.
Angewandte Chemie (International ed. in English), 51(52), 13062-13065 (2012-11-20)
The key step in this total synthesis of (-)-acetylaranotin is the efficient formation of the characteristic dihydrooxepine ring from cyclohexenone through an unusual vinylogous Rubottom oxidation and a regioselective Baeyer-Villiger oxidation. (-)-Acetylaranotin is obtained in 22 steps from commercially available
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
Julio H K Rozenfeld et al.
Biochimica et biophysica acta, 1848(1 Pt A), 127-133 (2014-10-16)
In this work, the bilayer structure of novel cationic lipid diC16-amidine was compared to the one of zwitterionic dipalmitoyl phosphatidylcholine ( DPPC), which shares the same hydrophobic domain. Differential scanning calorimetry shows that DPPC and diC16-am idine bilayers have similar
William Conway et al.
The journal of physical chemistry. A, 117(5), 806-813 (2013-01-05)
Piperazine (PZ) is widely recognized as a promising solvent for postcombustion capture (PCC) of carbon dioxide (CO(2)). In view of the highly conflicting data describing the kinetic reactions of CO(2)(aq) in piperazine solutions, the present study focuses on the identification
Niina Aaltonen et al.
Chemistry & biology, 20(3), 379-390 (2013-03-26)
Monoacylglycerol lipase (MAGL) terminates the signaling function of the endocannabinoid, 2-arachidonoylglycerol (2-AG). During 2-AG hydrolysis, MAGL liberates arachidonic acid, feeding the principal substrate for the neuroinflammatory prostaglandins. In cancer cells, MAGL redirects lipid stores toward protumorigenic signaling lipids. Thus MAGL
Christopher D Smith et al.
Clinical medicine (London, England), 14(4), 409-415 (2014-08-08)
The use of novel psychoactive substances ('legal highs' or 'designer drugs') is increasing worldwide. Patients misusing such substances have been reported to experience severe or prolonged side effects requiring admission to acute or critical care wards. These complications can be
Almeqdad Y Habashneh et al.
Archiv der Pharmazie, 347(6), 415-422 (2014-03-13)
A new series of N1-(flavon-6-yl)amidrazones were synthesized by reacting the hydrazonoyl chloride derived from 6-aminoflavone with the appropriate sec-cyclic amines. The antitumor activities of these compounds were evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines. Among the compounds
John R Lever et al.
The Journal of pharmacology and experimental therapeutics, 351(1), 153-163 (2014-08-08)
Psychostimulant effects of cocaine are mediated partly by agonist actions at sigma-1 (σ1) receptors. Selective σ1 receptor antagonists attenuate these effects and provide a potential avenue for pharmacotherapy. However, the selective and high affinity σ1 antagonist PD144418 (1,2,3,6-tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propylpyridine) has been
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
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
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
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
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
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
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
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
Sang-Yong Lee et al.
Biochemical pharmacology, 93(2), 171-181 (2014-12-03)
Polyoxometalates (POMs) are inorganic cluster metal complexes that possess versatile biological activities, including antibacterial, anticancer, antidiabetic, and antiviral effects. Their mechanisms of action at the molecular level are largely unknown. However, it has been suggested that the inhibition of several
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
Chen Liu et al.
Water research, 46(16), 5235-5246 (2012-08-07)
This study addressed the formation and properties of degradation products of ciprofloxacin, norfloxacin and lomefloxacin formed during ozonation of secondary wastewater effluent containing these fluoroquinolone antibiotics. The generation of the degradation products was interpreted in the context of transformations of
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