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    • Journal of Photopolymer Science and Technology Journal

    Papers
    Novel Bradykinin-1 Antagonists Containing a (1,2,3,4-Tetrahydro-isoquinolin-1-yl)acetic Acid Scaffold
    Jozsef Huszar,Zoltan Timar,Krisztina Katalin Szalai,Gyoergy Keserue,Ferenc Fueloep,Botond Penke
    European Journal of Medicinal Chemistry（2007）
    A novel B(1) antagonist core was utilized and the effects of modification of its amide side chain on the biological activity were tested. The imino functional group of isoquinolin-1-ylacetic acid and its 6,7-dimethoxy variant was sulfonylated (4-toluenesulfonyl), while the acetyl...
    Cited8Views11
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    The HIV-1 Maturation Inhibitor, EP39, Interferes with the Dynamic Helix-Coil Equilibrium of the CA-SP1 Junction of Gag
    Xiaowei Chen,Pascale Coric,Valery Larue,Serge Turcaud,Xiao Wang,Sylvie Nonin-Lecomte,Serge Bouaziz
    European Journal of Medicinal Chemistry（2020）
    During the maturation of HIV-1 particle, the Gag polyprotein is cleaved into several proteins by the HIV-1 protease. These proteins rearrange to form infectious virus particles. In this study, the solution structure and dynamics of a monomeric mutated domain encompassing the C-te...
    Cited7Views26
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    Preliminary Research on 1-(4-bromo-2-nitroimidazol-1-yl)-3-[18f]fluoropropan-2-ol As a Novel Brain Hypoxia PET Tracer in a Rodent Model of Stroke
    Elena Nieto,Mercedes Delgado,Monica Sobrado,Maria L. de Ceballos,Ramon Alajarin,Luis Garcia-Garcia,James Kelly,Ignacio Lizasoain,Miguel A. Pozo,Julio Alvarez-Builla
    European Journal of Medicinal Chemistry（2015）
    The synthesis of the new radiotracer precursor 4-Br-NITTP and the radiolabeling of the new tracer 1-(4-bromo-2-nitroimidazol-1-yl)-3-[18F]fluoropropan-2-ol (4-Br-[18F]FMISO) is reported. The cyclic voltammetry behaviour, neuronal cell toxicity, transport through the brain endothe...
    Cited7Views35
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    3,3′-Di[1,3-thiazolidin-4-one] System. Structural and Conformational Studies on Configurational Isomers with Anti-Inflammatory Activity
    Fulvia Orsini,Gabriella Bombieri,Franco Benetollo,M. Gabriella Vigorita,Tindara Previtera
    Journal of Chemical Crystallography（1995）
    The stereochemistry of the 3,3′-(1,2-ethanediyl)bis[2-(3-fluorophenyl)-1,3-thiazolidine-4-one] configurational isomers (2R,2′R2S,2′S and 2R,2′Smeso) has been investigated by 1H-NMR techniques in solution, by X-ray diffraction methods in the solid state and by quantum chemical met...
    Cited72Views3
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    Synthesis of Bicoumarin Thiophosphate Derivatives As Steroid Sulfatase Inhibitors
    Sebastian Demkowicz,Witold Kozak,Mateusz Dasko, Maciej Magyk,Bartlomiej Gielniewski,Janusz Rachon
    European Journal of Medicinal Chemistry（2015）
    Based on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologic...
    Cited20Views17
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    Synthesis and Antiproliferative Activity of Goniobutenolides A and B, 5-Halogenated Crassalactone D Derivatives and the Corresponding 7-Epimers
    Ivana Kovacevic,Mirjana Popsavin,Goran Benedekovic,Vesna Kojic,Dimitar Jakimov,Marko V. Rodic,Tatjana Srdic-Rajic,Gordana Bogdanovic,Vladimir Divjakovic,Velimir Popsavin
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY（2016）
    A new synthesis of goniobutenolides A (1) and B (2) and the corresponding 7-epimers has been achieved starting from diacetone d-glucose. The key step of the synthesis is a new one-pot sequence that commenced with Z-selective Wittig (or Horner-Wadsworth-Emmons) olefination, follow...
    Cited5Views31
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    Exploration of the Molecular Architecture of the Orthosteric Binding Site in the Α4β2 Nicotinic Acetylcholine Receptor with Analogs of 3-(Dimethylamino)butyl Dimethylcarbamate (DMABC) and 1-(Pyridin-3-yl)-1,4-diazepane
    Tinna B. Bach,Anders A. Jensen,Jette G. Petersen,Troels E. Sorensen,Serena Della Volpe, Jun Liu,Antoni R. Blaazer,Jacqueline E. van Muijlwijk-Koezen,Thomas Balle,Bente Frolund
    European Journal of Medicinal Chemistry（2015）
    X-ray crystal structures of acetylcholine binding proteins (AChBPs) have revealed two different possible extensions to the classical ligand binding pocket known to accommodate various nicotinic agonists. One of the pockets is limited in size while the other is of considerable dim...
    Cited3Views34
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    Novel Thiopyrano[3,2-B] and Cycloalkeno[1,2-B]Indole Derivatives with High Inhibitory Properties in Ltb4 Production
    C Kuehm-Caubere,P Caubere,B Jamart-Gregoire,B Pfeiffer, P Guardiola-Lemaitre,D Manechez,P Renard
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY（1999）
    Series of thiopyrano[3,2-b] and cycloalkeno[1,2-b]indoles were synthesized and evaluated in order to determine thenecessary structural requirements for high leukotrienes biosynthesis inhibition. In vitro experiments showed that compounds 11b and 12b belonging to the second series...
    Cited35Views9
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    Purine-benzimidazole Hybrids: Synthesis, Single Crystal Determination and in Vitro Evaluation of Antitumor Activities
    Alka Sharma,Vijay Luxami,Kamaldeep Paul
    European Journal of Medicinal Chemistry（2015）
    In an effort to identify novel compounds for the treatment of cancer, a diverse array of potential bioactive hybrid, purine-benzimidazole was synthesized in good yields through nucleophilic substitution at C6 position of purine ring with versatile cyclic amines at C2 position. Th...
    Cited40Views9
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    Synthesis of Some Novel Oxime Ether Derivatives and Their Activity in the 'behavioral Despair Test'
    O Bozdag,B Gumusel,R Demirdamar,E Buyukbingol,Y Rolland,R Ertan
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY（1998）
    In this study, a new series of 2-aminoethyloxime ether derivatives of some aralkylketones was synthesized. Their structures have been elucidated by UV, IR, H-1-NMR, C-13-NMR, mass spectra and elementary analysis. These compounds were then screened for their inhibition of immobili...
    Cited18Views6
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    Symbiotic Approach to Drug Design: N-[(4-chloro-3-sulfamoylbenzamido)-ethyl]propanolamine Derivatives As Β-Adrenergic Blocking Agents with Diuretic Activity
    V CECCHETTI,F SCHIAFFELLA,O TABARRINI, W ZHOU,A FRAVOLINI,A GOI,G BRUNI,G SEGRE
    European Journal of Medicinal Chemistry（1991）
    A series of oxypropanolamines and iminoxypropanolamines, in which the aminic substituent was the 2-(4-chloro-3-sulfamoylbenzamido)-ethyl group, were synthesized as potential β-blocker/diuretic agents. All of these compounds were tested for β1-adrenoceptor affinity and β-blocking ...
    Cited11Views8
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    Synthesis and Biological Evaluation of New 4H-Pyrano[2,3-b]quinoline Derivatives That Block Acetylcholinesterase and Cell Calcium Signals, and Cause Neuroprotection Against Calcium Overload and Free Radicals
    Jose Marco-Contelles,Rafael Leon,Manuela G. Lopez,Antonio G. Garia,Mercedes Villarroya
    European Journal of Medicinal Chemistry（2006）
    The synthesis and biological evaluation of ethyl 5-amino-4-(3-pyridyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrano[2,3-b]quinoline-3-carboxylates (9-11) is described. We have found that these compounds inhibit AChE with a mild potency, mitigates the [Ca(2+)](c) triggered by high K(+), ...
    Cited57Views3
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    Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors
    Yan Xia,Hyun-Kyung Choi,Kyeong Lee
    European Journal of Medicinal Chemistry（2012）
    Tumor hypoxia has been recognized as a common feature of solid tumors and a negative prognostic factor for response to treatment and survival of cancer patients. The discovery of hypoxia-inducible factor-1 (HIF-1), a molecular determinant of responses to hypoxia in mammalian cell...
    Cited269Views20
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