Browsing Research publications by Author "Medicinal and Analytical Chemistry"
Now showing items 1-20 of 162
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2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections
Tasdemir, Deniz; Sanabria, David; Lauinger, Ina L; Tarun, Alice; Herman, Rob; Perozzo, Remo; Zloh, Mire; Kappe, Stefan H.; Brun, Reto; Carballeira, Néstor M (2010)Acetylenic fatty acids are known to display several biological activities, but their antimalarial activity has remained unexplored. In this study, we synthesized the 2-, 5-, 6-, and 9-hexadecynoic acids (HDAs) and evaluated ... -
2β-Acetoxyferruginol - A new antibacterial abietane diterpene from the bark of Prumnopitys andina
Smith, E.C.J.; Gibbons, S.; Wareham, N.; Zloh, Mire (2008-04-15)As part of an on-going project to isolate antibacterial compounds from rare conifer species, a new abietane diterpene, 2β-acetoxyferruginol was isolated from the stem bark of Prumnopitys andina. Molecular modelling studies ... -
4,4’-dimethylaminorex (‘4,4’-DMAR’; ‘Serotoni’) misuse; a web-based study
Loi, Barbara; Zloh, Mire; Antonietta, Maria; Corkery, John; Schifano, Fabrizio (2017-06-28)Background: 4,4′-DMAR (4,4’-dimethylaminorex; ‘Serotoni’) is a potent stimulant drug which has recently been associated with a number of fatalities in Europe. Over the last few years, online communities have emerged as ... -
5,6-Methylenedioxy-2-aminoindane : from laboratory curiosity to 'legal high'
Gallagher, C. T.; Assi, S.; Stair, J. L.; Fergus, S.; Corazza, Ornella; Corkery, John; Schifano, Fabrizio (2012-03-01)The fully synthetic 'legal high' 5,6-methylenedioxy-2-aminoindane (MDAI) is an analogue of 3,4-methylenedioxymethamphetamine. Although developed in the 1990s, it was not widely abused until 2010. However, mephedrone was ... -
Accelerated metabolite identification by "Extraction-NMR"
Gerhard, U.; Thomas, S.; Mortishire-Smith, R. (2003-07-14)Examples of the use of extraction-NMR, an efficient and rapid method to obtain structural information on metabolites without prior separation, are described. Crude ethyl acetate extracts of in vitro microsomal incubations ... -
Acid unfolding of beta-2-microglobulin by repulsion of + charges
Bray, P.; Vucic, M.; Zloh, Mire; Vucelic, D. (1988-07) -
Aconityl-derived polymers for biomedical applications : Modeling study of cis-trans isomerisation
Zloh, Mire; Dinand, E.; Brocchini, S. (2003-05-01)Soluble polymers have been prepared that are designed to undergo enhanced rates of hydrolysis at pH values less than that observed in blood circulation. The degradable element in the polymer mainchain is derived from ... -
Advanced microscopy solutions for monitoring the kinetics and dynamics of drug-DNA targeting in living cells
Errington, Rachel J.; Ameer-Beg, S. M.; Vojnovic, B.; Patterson, Laurence H.; Zloh, Mire; Smith, P. J. (2005)Many anticancer drugs require interaction with DNA or chromatin components of tumor cells to achieve therapeutic activity. Quantification and exploration of drug targeting dynamics can be highly informative in the rational ... -
Amanicadol, a pimarane-type diterpene from Phlomis amanica Vierch
Yalçin, F.N.; Ersöz, T.; Çaliş, I.; Bedir, E.; Dönmez, A.A.; Stavri, M.; Gibbons, S.; Zloh, Mire (2006-11-01)Fractionation of the methanol extract of Phlomis amanica resulted in the isolation of a new pimarane type diterpene, amanicadol (1), together with the known glycosides lamiide, verbascoside (= acteoside), syringaresinol-4-O-β- ... -
Analysis of histones from the yeast Saccharomyces carlsbergensis
Pastink, A.; Berkhout, Theo; Mager, W.H.; Planta, R.J. (1979-02)Basic chromosomal proteins were isolated from the chromatin of the yeast Saccharomyces carlsbergensis by extraction with H2SO4 and were purified by ion-exchange chromatography. Electrophoresis of the purified fraction on ... -
An analysis of the 'legal high' mephedrone
Gibbons, Simon; Zloh, Mire (2010)'Legal highs' are compounds, plant or fungal material which can be readily bought from the internet without legal restriction and the single chemicals may be structurally related to illegal drugs of abuse such as the ... -
Antagonistic effects of indoloquinazoline alkaloids on antimycobacterial activity of evocarpine
Hochfellner, C.; Evangelopoulos, D.; Zloh, Mire; Wube, A.; Guzman, J. D.; Mchugh, T. D.; Kunert, O.; Bhakta, S.; Bucar, F. (2015-04-01)The interaction of quinolone and indoloquinazoline alkaloids concerning their antimycobacterial activity was studied. Methods and Results: The antimycobacterial and modulating activity of evodiamine (1), rutaecarpine (2) ... -
Antibacterial acylphloroglucinols from Hypericum olympicum
Shiu, Winnie K. P.; Rahman, M. Mukhlesur; Curry, Jonathan; Stapleton, Paul; Zloh, Mire; Malkinson, John P.; Gibbons, Simon (2012)New antibacterial acylphloroglucinols (1-5) were isolated and characterized from the aerial parts of the plant Hypericum olympicum L. cf. uniflorum. The structures of these compounds were confirmed by extensive 1D- and ... -
Application of diffusion-edited and solvent suppression 1H NMR to the direct analysis of markers in valerian-hop liquid herbal products
Prieto, Jose M.; Mellinas-Gomez, Maria; Zloh, Mire (2016-03-01)The rising trend to consume herbal products for the treatment and/or prevention of minor ailments together with their chemical and pharmacological complexity means there is an urgent need to develop new approaches to their ... -
Arene-fused 1,2-oxazole N-oxides and derivatives. The impact of the N-O dipole and substitution on their aromatic character and reactivity profile. Can it be a useful structure in synthesis? A theoretical insight
Kozielewicz, Paweł; Tzeli, Demeter; Tsoungas, Petros G.; Zloh, Mire (2014-12-01)DFT calculations have shown that the N-O dipole of benzene- and naphthalene-fused 1,2-oxazole N-oxides causes a distortion of their σ and π frame, concentrated on the 1,2-oxazole ring, such that it increases its susceptibility ... -
Aryldiketo acids have antibacterial activity against MDR Staphylococcus aureus strains : Structural insights based on similarity and molecular interaction fields
Drakulić, B.J.; Stavri, M.; Gibbons, S.; Žižak, Ž.S.; Verbić, T.Ž.; Juranić, I.O.; Zloh, Mire (2009-12-07)(Chemical Equation Presented) Similar structure=similar activity? The effect of substituents on the antibacterial activity of aryldiketo acids has been rationalised by molecular interaction fields and similarity studies ... -
Bioadhesive tablets containing cyclodextrin complex of Itraconazole for the treatment of vaginal candidiasis
Cevher, Erdal; Açma, Ayşe; Sinani, Genada; Aksu, Buket; Zloh, Mire; Mülazımoğlu, Lütfiye (2014-08)Itraconazole (ITR) is commonly used in the treatment of Candida infections. It has a nephrotoxic effect and low bioavailability in patients who suffer from renal insufficiency, and its poor solubility in water makes ITR ... -
C9orf72 hexanucleotide repeat associated with amyotrophic lateral sclerosis and frontotemporal dementia forms RNA G-quadruplexes
Fratta, Pietro; Mizielinska, Sarah; Nicoll, Andrew J; Zloh, Mire; Fisher, Elizabeth M. C.; Parkinson, Gary; Isaacs, Adrian M. (2012)Large expansions of a non-coding GGGGCC-repeat in the first intron of the C9orf72 gene are a common cause of both amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). G-rich sequences have a propensity ... -
Cationic Poly-l-lysine Dendrimer Complexes Doxorubicin and Delays Tumor Growth in Vitro and in Vivo
Al-Jamal, Khuloud; Al-Jamal, Wafa; Wang, Julie T.-W.; Rubio, Noelia; Buddle, Joanna; Gathercole, David; Zloh, Mire; Kostarelos, Kostas (2013)We report in this study the complexation of the chemotherapeutic drug doxorubicin (DOX) with the novel sixth-generation cationic poly-l-lysine dendrimer (DM) (MW 8149 kDa), which we previously reported to exhibit systemic ... -
CCR2: Characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach
Berkhout, Theo; Blaney, F.E.; Bridges, A.M.; Cooper, D.G.; Forbes, I.T.; Gribble, A.D.; Groot, P.H.E.; Hardy, A.; Ife, R.J.; Kaur, R.; Moores, K.E.; Shillito, H.; Willetts, J.; Witherington, J. (2003-09-11)We describe here a classical molecular modeling exercise that was carried out to provide a basis for the design of novel antagonist ligands of the CCR2 receptor. Using a theoretical model of the CCR2 receptor, docking ...