- BIVALENT LECA INHIBITORS TARGETING BIOFILM FORMATION OF PSEUDOMONAS AERUGINOSA
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The present invention relates to divalent compounds binding to LecA. The compounds are useful to block biofilm formation of Pseudomonas aeruginosa. The invention further relates to pharmaceutical compositions comprising these compounds and to therapeutic methods and uses of these compounds, in particular to therapeutic methods and uses for the treatment of Pseudomonas aeruginosa infections in a subject. The invention also relates to imaging of infections, such as biofilms produced by Pseudomonas aeruginosa, by using these divalent compounds.
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Page/Page column 45; 48-49; 50
(2021/05/15)
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- Discovery of Diphenoxy Derivatives with Flexible Linkers as Ligands for β-Amyloid Plaques
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The highly rigid and planar scaffolds with π-conjugated systems have been widely considered to be indispensable for β-amyloid (Aβ) binding ligands. In this study, a library of diphenoxy compounds with different types of more flexible linkers as Aβ ligands were synthesized and evaluated. Most of them displayed good affinity (Ki1-42aggregates, and some ligands even showed values of Kiless than 10 nM. Structure-activity relationship analysis revealed that modification on the linkers or substituents tolerated great flexibility, which challenged the long-held belief that rigid and planar structures are exclusively favored for Aβ binding. Three ligands were labeled by iodine-125, and they exhibited good properties in vitro and in vivo, which further supported that this flexible scaffold was potential and promising for the development of Aβ imaging agents.
- Jia, Jianhua,Zhang, Longfei,Song, Jia,Dai, Jiapei,Cui, Mengchao
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p. 4089 - 4100
(2020/12/13)
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- Design and characterization of novel bis-benzamide liquid crystalline materials
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A new homologous series of symmetric, bent-shaped bis-benzamide dimers have been prepared. Several 1,n-bis(p-aminophenoxy)alkanes (n = 3, 5, 9,10,11) were employed as spacers and p-hexyloxy tails have been synthesized and appended to the spacers by amide linking groups. Different important parameters were explored using computational analysis by semi empirical method. The experimental results were correlated with theoretical studies and relationship between molecular structure and mesogenic behavior has been established. The mesomorphic properties of the resultant dimers were characterized by differential scanning calorimetry (DSC) and polarized optical microscopy (POM) equipped with a hot stage. Change in mesomorphic properties with change of methylene spacers was observed. Enantiotropic mesogenic behavior was exhibited by D3A6, D10A6 and D11A6 and the needle like and blurred schleiren textures were observed. It was observed that increased methylene spacers chain length decreased the melting temperatures. Thermogravimetric analysis revealed the thermal stability of dimers upto 360 °C.
- Iqbal, Asma,Siddiqi, Humaira Masood,Akhter, Zareen,Qaiser Fatmi, Muhammad
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p. 135 - 141
(2017/09/23)
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- Synthesis and Thermal Studies of Some Epoxy Systems cured with Aromatic Diamines
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Some aromatic diamines having flexible ether linkages with variable aliphatic and aromatic character were synthesized via Williamson's method and used as curing agents in their solution phase and/or molten state for a commercially available epoxy resin; diglycidyl ether of bisphenol-A (DGEBA) (n = 0.03, epoxy equivalent = 174.5 g/mol). The resulting polymeric systems were characterized by their physical properties and FT-IR-spectral studies. The thermal behaviour of the synthesized epoxy polymers were evaluated by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). The optimum curing temperature of these polymers was found to be ~ 150°C. The polymers were stable up to 270°C with maximum weight loss at ~ 400°C.
- Khalid, Naila,Khan, Muhammad Saif Ullah,Siddiqi, Humaira Masood,Akhter, Zareen,Iqbal, Naseer
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p. 570 - 577
(2012/01/03)
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- Synthesis and characterization of new optically active poly(amide-imide)s based on n-trimellitimido-l-amino acid and trimethylene units
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Six new optically active poly(amide-imide)s (8a-f) were synthesized through the direct polycondensation reaction of 1,3-bis(4-aminophenoxy) propane (4) with six different derivatives of N-trimellitimido-L-amino acid (7a-f) in a medium consisting of N-meth
- Faghihi, Khalil,Shabanian, Meisam
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scheme or table
p. 97 - 102
(2012/05/20)
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- QSAR modeling, synthesis and bioassay of diverse leukemia RPMI-8226 cell line active agents
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A rigorous QSAR modeling procedure employing CODESSA PRO descriptors has been utilized for the prediction of more efficient anti-leukemia agents. Experimental data concerning the effect on leukemia RPMI-8226 cell line tumor growth of 34 compounds (treated
- Katritzky, Alan R.,Girgis, Adel S.,Slavov, Svetoslav,Tala, Srinivasa R.,Stoyanova-Slavova, Iva
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experimental part
p. 5183 - 5199
(2011/01/04)
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- Synthesis of symmetric liquid crystal dimers based on azo and imine groups and investigation of phase behaviour by varying alkoxy terminal chain length
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With the objective to study the effect of alkoxy terminal chain length on mesomorphic properties of liquid crystals, we have synthesized two (Azo and Imine) different series of dimesogens by varying terminal alkoxy chain length (n = 6-12) with a short spacer unit in between two mesogens. Transition temperatures and phase characterization were studied by DSC, POM and XRD analysis. It was found that all the dimers show mesomorphic properties and the change in terminal alkoxy chain length has pronounced effect on the smectic phase window. In the DSC cooling scan, the smectic phase window of azo compounds increased from 6.4°C (2A6) to 16.0°C(2A12), whereas in Schiff base compounds, it increased from 9.2°C (2S6) to 31.0°C(2S12). Further, the 2A11 dimer was found to undergo photo induced configurational changes.
- Kim, Tae Hyeong,Lee, Chang Sin,Ramaraj,Jeon, Hye Jin,Song, Hyun Hoon,Lee, Soo Min,Yoon, Kuk Ro
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experimental part
p. 102 - 116
(2010/03/04)
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- Synthesis, characterization and ion transportation studies of some novel cyclophane amides
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Various novel cyclophane amides with a large cavity have been synthesized. The structures of cyclophane amides 14 and 15 were resolved using XRD studies. Cyclophane amide 28 shows a shift in λmax in the UV/Vis. spectra when treated with Cu (II) ion as well as with Pb (II) ion. Ion transportation studies were carried out with cyclophane amide 14 which proved that the Na+ ion passes through the cavity while K+ ions are retained.
- Rajakumar, Perumal,Rasheed, A. Mohammed Abdul
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p. 5351 - 5362
(2007/10/03)
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- Biological properties of amidinium sulfinic and sulfonic acid derivatives: inhibition of glycolytic enzymes of Trypanosoma brucei and protective effect on cell growth
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The activity of the title compounds has been investigated on two biological targets: cultures of trypanosome and glycolytic enzymes inhibition of the parasite, and on retinal epithelium cells.In both cases, these compounds exhibit a significant activity,
- Willson, M,Perie, JJ,Malecaze, F,Opperdoes, F,Callens, M
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p. 799 - 808
(2007/10/02)
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- Process for preparing substituted bis-ethers
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Substituted bis-ethers, such as α,107 -bis-(4-aminophenoxy)-alkyls, are prepared in process which involves sequential addition of reactants, reagents or neutralizing compounds without recovery of intermediate products such as diamides and diamine acid sal
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- Novel Bis as Antitrypanosomal Agents
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A series of novel 1,1'-(4,1-phenylene)bis was prepared and evaluated for activity against Trypanosoma rhodesiense in mice.The importance of the bis structure and the nature of the spacer between the two phenyl rings for optimal activity have been revealed.The potent parenteral activity of several analogues within this series as well as preliminary indication of oral activity lends encouragement to further development of this structural class.
- Turner, William R.,Werbel, Leslie M.
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p. 1728 - 1740
(2007/10/02)
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- MESOGENIC POLYMERS. 6. TWO SERIES OF ISOMERIC POLYAZOMETHINES.
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Two homologoous series of alternating rigid-flexible, main chain liquid crystalline polyimines are reported; one based on terephthaldehyde the other based on p-phenylenediamine. It was found through examination of optical microscopic, x-ray diffraction an
- Griffin,Britt,Hung,Steele
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p. 305 - 314
(2007/10/02)
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- Poly(6-oxy-2,2,4-trialkyl-1,2-dihydroquinoline)alkylene compounds as antidegradants for rubber
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Vulcanizable or vulcanized diene elastomers containing stabilizing amounts of certain poly(6-oxy-2,2,4-trialkyl-1,2-dihydroquinoline)alkylene antidegradants show resistance to ozone attack. The antidegradants themselves are novel compounds.
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