53 (s, 1H, NNHCO)73 (br s, 1H, NH, Ar). 13 C NMR (DMSOd 6 )?: 31.95 (CH 2 CH=), p.7449 ,
66 (s, 2H, CH 2 CONH), Ar NHCO, vol.34387, issue.11, pp.29-36 ,
15 (s, 1H, NNHCO)72 (br s, 1H, H- 1, NH, Ar). 13 C NMR (DMSO-d 6 ) ?: 30, CH=, vol.11, issue.12 2, p.36 ,
6708(13)Å, ? = 75647 g cm ?3 , ? = 4.815 mm ?1 . The structure was solved by direct methods using the SIR97 program [46], and then refined with full-matrix least-square methods based on F 2 (SHELXL-97) [47] with the aid of the WINGX [48]program. The contribution of the disordered solvents to the calculated structure factors was estimated following the BYPASS algorithm [49], implemented as the SQUEEZE option in PLATON [50]. A new data set, free of solvent contribution, was then used in the final refinement. All non-hydrogen atoms were refined with anisotropic atomic displacement parameters. H atoms were finally included in their calculated positions. A final refinement on F 2 with 8064 unique intensities and 361 parameters converged at ?R(F 2 )) for 2888 observed reflections with I > 2? (I) Crystallographic data for the structure of 3a in this paper have been deposited in the Cambridge Crystallographic Data Centre as supplementary publication number CCDC 938832. Copies of the data can be obtained, free of charge, on application to CCDC, ?g heparin/mL. Buffer B 50 mM MgCl 2 , 90 mM NaCl, p.50, 1771. ,
Long-Term Clinical Effects of Epalrestat, an Aldose Reductase Inhibitor, on Diabetic Peripheral Neuropathy: The 3-year, multicenter, comparative Aldose Reductase Inhibitor-Diabetes Complications Trial, Diabetes Care, vol.29, issue.7, pp.1538-154410, 2006. ,
DOI : 10.2337/dc05-2370
Aldose reductase structures: implications for mechanism and inhibition, Cell Mol Life Sci, vol.61, pp.750-752, 2004. ,
New cholesterol esterase inhibitors based on rhodanine and thiazolidinedione scaffolds, Bioorganic & Medicinal Chemistry, vol.19, issue.24, pp.7453-7463, 2011. ,
DOI : 10.1016/j.bmc.2011.10.042
Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-x L, Nature Cell Biology, vol.3, issue.2, pp.173-1821035055085, 1038. ,
DOI : 10.1038/35055085
Development of dimeric modulators for anti-apoptotic Bcl-2 proteins, Bioorganic & Medicinal Chemistry Letters, vol.18, issue.1, 2008. ,
DOI : 10.1016/j.bmcl.2007.10.088
Enhanced Fidelity in Mismatch Extension by DNA Polymerase through Directed Combinatorial Enzyme Design, Angewandte Chemie International Edition, vol.391, issue.30, pp.4712-4715, 2005. ,
DOI : 10.1002/anie.200500047
Small Molecule Inhibitors of Human DNA Polymerase ??, ACS Chemical Biology, vol.6, issue.4, pp.314-319, 2011. ,
DOI : 10.1021/cb100382m
Development of Tau Aggregation Inhibitors for Alzheimer's Disease, Angewandte Chemie International Edition, vol.282, issue.10, pp.1740-1752, 2009. ,
DOI : 10.1002/anie.200802621
Tau protein and tau aggregation inhibitors, Neuropharmacology, vol.59, issue.4-5, pp.276-289, 2010. ,
DOI : 10.1016/j.neuropharm.2010.01.016
Small-Molecule Inhibitors of Islet Amyloid Polypeptide Fibril Formation, Angewandte Chemie International Edition, vol.300, issue.25, pp.4679-4682, 2008. ,
DOI : 10.1002/anie.200705372
Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D, Bioorganic & Medicinal Chemistry Letters, vol.6, issue.18, pp.2157-2162, 1996. ,
DOI : 10.1016/0960-894X(96)00393-9
Enoyl-Acyl Carrier Protein Reductase, Journal of Medicinal Chemistry, vol.50, issue.11, pp.2665-2675, 2007. ,
DOI : 10.1021/jm061257w
Identification of Inhibitors for UDP-Galactopyranose Mutase, Journal of the American Chemical Society, vol.126, issue.34, pp.10532-10533, 2004. ,
DOI : 10.1021/ja048017v
SAR and Mode of Action of Novel Non-Nucleoside Inhibitors of Hepatitis C NS5b RNA Polymerase, Journal of Medicinal Chemistry, vol.49, issue.3, pp.1034-104610, 1021. ,
DOI : 10.1021/jm050859x
Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors, Bioorganic & Medicinal Chemistry Letters, vol.19, issue.13, pp.3615-3618, 2009. ,
DOI : 10.1016/j.bmcl.2009.04.132
??-Diketo Acid Pharmacophore Hypothesis. 1. Discovery of a Novel Class of HIV-1 Integrase Inhibitors, Journal of Medicinal Chemistry, vol.48, issue.1, pp.111-120, 2005. ,
DOI : 10.1021/jm0496077
Recent Advances on Phosphodiesterase 4 Inhibitors for the Treatment of Asthma and Chronic Obstructive Pulmonary Disease, Journal of Medicinal Chemistry, vol.51, issue.18, pp.5471-5885, 2008. ,
DOI : 10.1021/jm800582j
Rhodanine derivatives as selective protease inhibitors against bacterial toxins, Chem Biol Drug Des, vol.71, pp.131-139, 2008. ,
Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors, European Journal of Medicinal Chemistry, vol.45, issue.2, pp.805-810, 2010. ,
DOI : 10.1016/j.ejmech.2009.10.009
URL : https://hal.archives-ouvertes.fr/hal-00869769
Leucettines, a Class of Potent Inhibitors of cdc2-Like Kinases and Dual Specificity, Tyrosine Phosphorylation Regulated Kinases Derived from the Marine Sponge Leucettamine B: Modulation of Alternative Pre-RNA Splicing, Journal of Medicinal Chemistry, vol.54, issue.12, pp.4172-418610, 1021. ,
DOI : 10.1021/jm200274d
URL : https://hal.archives-ouvertes.fr/hal-00870007
Selectivity, Cocrystal Structures, and Neuroprotective Properties of Leucettines, a Family of Protein Kinase Inhibitors Derived from the Marine Sponge Alkaloid Leucettamine B, Journal of Medicinal Chemistry, vol.55, issue.21, pp.9312-933010, 1021. ,
DOI : 10.1021/jm301034u
URL : https://hal.archives-ouvertes.fr/hal-00870472
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines, European Journal of Medicinal Chemistry, vol.62, 2013. ,
DOI : 10.1016/j.ejmech.2013.01.035
URL : https://hal.archives-ouvertes.fr/hal-00822733
Dispacamides, anti-histamine alkaloids from Caribbean Agelas sponges, Tetrahedron Letters, vol.37, issue.20, pp.3587-359010, 1996. ,
DOI : 10.1016/0040-4039(96)00629-6
An efficient approach to dispacamide A and its derivatives, Org. Biomol. Chem., vol.38, issue.5, pp.978-987, 2012. ,
DOI : 10.1039/C1OB06161E
URL : https://hal.archives-ouvertes.fr/hal-00870469
Ultrasound and microwave: recent advances in organic chemistry, Research Signpost, Kerala, 2011. ,
Microwave-assisted synthesis of novel bis(2-thioxothiazolidin-4-one) derivatives as potential GSK-3 inhibitors, Tetrahedron Letters, vol.53, issue.31, pp.3998-4003, 2012. ,
DOI : 10.1016/j.tetlet.2012.05.088
Aqueous microwave-assisted one-pot synthesis of N-substituted rhodanines, Tetrahedron Letters, vol.53, issue.39, pp.5197-5201, 2012. ,
DOI : 10.1016/j.tetlet.2012.07.002
New cholesterol esterase inhibitors based on rhodanine and thiazolidinedione scaffolds, Bioorganic & Medicinal Chemistry, vol.19, issue.24, pp.7453-7463, 2011. ,
DOI : 10.1016/j.bmc.2011.10.042
New benzimidazoles as thrombopoietin receptor agonists, Bioorganic & Medicinal Chemistry Letters, vol.16, issue.5, pp.1212-1216, 2006. ,
DOI : 10.1016/j.bmcl.2005.11.096
Synthesis and biological evaluation of new glutamic acid-based inhibitors of MurD ligase, Bioorganic & Medicinal Chemistry Letters, vol.19, issue.1, pp.153-157, 2009. ,
DOI : 10.1016/j.bmcl.2008.10.129
Synthesis and antibacterial activity of 5-ylidenethiazolidin-4-ones and 5-benzylidene-4,6-pyrimidinediones, European Journal of Medicinal Chemistry, vol.45, issue.4, pp.1667-1672, 2010. ,
DOI : 10.1016/j.ejmech.2009.12.030
Discovery of Novel 5-Benzylidenerhodanine and 5-Benzylidenethiazolidine-2,4-dione Inhibitors of MurD Ligase, Journal of Medicinal Chemistry, vol.53, issue.18, pp.6584-659410, 1021. ,
DOI : 10.1021/jm100285g
New 5-benzylidenethiazolidin-4-one inhibitors of bacterial MurD ligase: Design, synthesis, crystal structures, and biological evaluation, European Journal of Medicinal Chemistry, vol.46, issue.11, pp.5512-5523, 2011. ,
DOI : 10.1016/j.ejmech.2011.09.017
Synthesis and biological evaluation of thiazolidine-2,4-dione and 2,4-thione derivatives as inhibitors of translation initiation, Bioorganic & Medicinal Chemistry Letters, vol.14, issue.21, pp.5401-5405, 2004. ,
DOI : 10.1016/j.bmcl.2004.08.017
Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D, Bioorganic & Medicinal Chemistry Letters, vol.6, issue.18, pp.2157-2162, 1996. ,
DOI : 10.1016/0960-894X(96)00393-9
Synthesis and characterization of (Z )-5- arylmethylidenerhodanines with photosynthesis-inhibiting properties, Molecules, vol.163390, pp.5207-522710, 2011. ,
ChemInform Abstract: A Solvent-Free Protocol for the Green Synthesis of Arylalkylidene Rhodanines in a Task-Specific Ionic Liquid., ChemInform, vol.88, issue.47, pp.514-518, 2010. ,
DOI : 10.1002/chin.201047123
Green synthesis of 5-benzylidene rhodanine derivatives catalyzed by 1-butyl-3-methyl imidazolium hydroxide in water, Monatshefte f??r Chemie - Chemical Monthly, vol.7, issue.8, pp.913-915, 2008. ,
DOI : 10.1007/s00706-008-0871-y
Synth??se de nouvelles spiro-rhodanine-pyrazolines par addition dipolaire-1,3 de la diphe??nylnitrilimine sur quelques 5-arylid??nerhodanines en ???milieu sec??? et sous irradiation micro-onde, New Journal of Chemistry, vol.22, issue.8, pp.809-81210, 1039. ,
DOI : 10.1039/a803447h
Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor, Bioorganic & Medicinal Chemistry Letters, vol.11, issue.2, pp.91-94, 2001. ,
DOI : 10.1016/S0960-894X(00)00610-7
97: a new tool for crystal structure determination and refinement, Journal of Applied Crystallography, vol.32, issue.1, pp.115-119, 1999. ,
DOI : 10.1107/S0021889898007717
suite for small-molecule single-crystal crystallography, Journal of Applied Crystallography, vol.32, issue.4, pp.837-838194, 1107. ,
DOI : 10.1107/S0021889899006020
Indirubins Inhibit Glycogen Synthase Kinase-3beta and CDK5/P25, Two Protein Kinases Involved in Abnormal Tau Phosphorylation in Alzheimer's Disease. A PROPERTY COMMON TO MOST CYCLIN-DEPENDENT KINASE INHIBITORS?, Journal of Biological Chemistry, vol.276, issue.1, pp.251-260, 2001. ,
DOI : 10.1074/jbc.M002466200
Purification of GSK-3 by Affinity Chromatography on Immobilized Axin, Protein Expression and Purification, vol.20, issue.3, pp.394-404, 2000. ,
DOI : 10.1006/prep.2000.1321
Purification of CK1 by affinity chromatography on immobilised axin, Protein Expression and Purification, vol.54, issue.1, pp.101-109, 2007. ,
DOI : 10.1016/j.pep.2007.02.020
URL : https://hal.archives-ouvertes.fr/hal-00169405