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Sonnet Pascal  - - - 
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Sylvain Routier

111 shared publications

A ICOA, UMR CNRS 7311 , University of Orleans , Orleans , France

Grace Gosmann

95 shared publications

Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil

Filomena Rossi

46 shared publications

Department of Pharmacy and CIRPeB, Università Federico II, 80134 Naples, Italy;(D.T.);(A.A.);(C.D.);(V.M.)

Catherine Mullié

42 shared publications

Laboratoire des Agents Infectieux, Resistance et Chimiothérapie – EA 4294, UFR de Pharmacie, Université de Picardie Jules Verne, Amiens, France

Mathieu Marchivie

23 shared publications

Univ. Bordeaux, ICMCB CNRS-UPR 9048, Pessac Cedex, France

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Distribution of Articles published per year 
(2007 - 2018)
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6
 
Publications
Article 2 Reads 0 Citations Crystal structure and identification of a pyrimido[6,1-b][1,3]oxazin-6-one derivative from the reaction of acrolein with... Jean Guillon, Sandra Rubio, Solène Savrimoutou, François Hal... Published: 01 November 2018
Comptes Rendus Chimie, doi: 10.1016/j.crci.2018.09.013
DOI See at publisher website ABS Show/hide abstract
The X-ray crystal structure of 2-(4,5-dihydro-5-phenoxymethyl-1,3-oxazol-2-ylamino)-7-(2-hydroxy-3-phenoxypropyl)hexahydro-2H,6H-pyrimido[6,1-b][1,3]oxazin-6-one (1), a structure of adduct formed by the reaction of 5-(phenoxymethyl)-2-amino-2-oxazoline and acrolein, has been established. The present work deals with the structural identification of the adduct 1 and presents a plausible mechanism for its formation. It crystallizes in the monoclinic space group P21/c with cell parameters a = 21.3337 (10) Å, b = 11.3712 (7) Å, c = 10.4936 (7) Å, β = 103.041 (3), V = 2480.0 (3) Å3, Z = 4. C26H32N4O6, Dc = 1.330 g/cm3, μ (Cu Kα) = 1.5418 Å, S = 1.188, F (000) = 1056, R = 0.0501, and wR = 0.1584. La structure complète de la 2-(4,5-dihydro-5-phénoxymethyl-1,3-oxazol-2-ylamino)-7-(2-hydroxy-3-phénoxypropyl)hexahydro-2H,6H-pyrimido[6,1-b][1,3]oxazin-6-one 1, une structure d'adduit formée lors de la réaction de la 5-(phénoxyméthyl)-2-amino-2-oxazoline et de l'acroléine, a été établie sans équivoque par une analyse cristallographique aux rayons X. Le présent travail porte sur l'identification structurale de l'adduit 1 et présente un mécanisme plausible pour sa formation. La molécule cristallise dans le système monoclinique, dans le groupe spatial P21/c avec a = 21.3337 (10) Å, b = 11.3712 (7) Å, c = 10.4936 (7) Å, β = 103.041 (3), V = 2480.0 (3) Å3, Z = 4. C26H32N4O6, Dc = 1.330 g/cm3, μ (Cu Kα) = 1.5418 Å, S = 1.188, F (000) = 1056, R = 0.0501 et wR = 0.1584.
PROCEEDINGS-ARTICLE 12 Reads 0 Citations Novel Racemic and Enantiopure Amino-Fluorene-Methanol Coumponds with Antimalarial Activities Jeremy Schneider, Alexandra Dassonville-Klimpt, Catherine De... Published: 01 November 2017
Proceedings of 3rd International Electronic Conference on Medicinal Chemistry, doi: 10.3390/ecmc-3-04653
DOI See at publisher website ABS Show/hide abstract
Malaria is a neglected tropical disease that remains a leading cause of morbidity and mortality among the world’s poorest populations. More than 100 tropical and sub-tropical countries are endemic for this infectious disease. Pregnant women and children are the most sensitive to this infection and, in 2015, 429 000 people died. Among the five species of Plasmodium responsible for human malaria, P. falciparum is the parasite which causes the most serious form of the disease. More recent efforts focused on the development of antimalarial vaccines and since 2001, World Health Organization (WHO) recommends artemisinin-based combination therapies (ACTs). In drugs resistance areas, several antimalarial drugs, such as aminoalcohol-aryl (mefloquine (MQ), lumefantrine (LM)), are currently used in combination with artemisinin derivatives. However, the emergence of multi-drug-resistant parasites decreases efficacy of ACTs. Thus, the design of new active compounds on Plasmodium-resistant strains is urgent. We have previously developed an asymmetric synthesis to prepare 4-aminoalcohol-quinoline enantiomers (AQ) as MQ analogs. They were active on nanomolar range against 3D7 (chloroquine-sensitive) and W2 (chloroquine-resistant) P. falciparum strains. Interestingly, (S)-enantiomers displayed an activity increased by 2 to 15-fold as compared to their (R)-counterparts. During the Plasmodium intra-erythrocytic asexual stages, hemozoin formation and the oxidative and glutathione-dependent degradation of heme are inhibited by these aminoalcohol-aryls (MQ, LM). Currently, their mechanisms of actions are not totally clear and remain to be explored. In continuation of our work, we are interested to study the change of heterocycle (fluorene vs quinoline) on the antimalarial activity. We focus on the design and the preparation of novel racemic and enantiopure aminoalcohol-fluorene derivatives (AFM) as LM analogs. The evaluation of their antiplasmodial activity against P. falciparum and their corresponding cytotoxicity is under progress.
Article 0 Reads 3 Citations Synthesis and Antiproliferative Effect of Ethyl 4-[4-(4-Substituted Piperidin-1-yl)]benzylpyrrolo[1,2-a ]quinoxalinecarb... Vanessa Desplat, Marian Vincenzi, Romain Lucas, Stéphane Mor... Published: 05 April 2017
ChemMedChem, doi: 10.1002/cmdc.201700049
DOI See at publisher website PubMed View at PubMed
PROCEEDINGS-ARTICLE 9 Reads 0 Citations Synthesis of Fluorenes with Potential Bioactivities Schneider Jeremy, Dassonville-Klimpt Alexandra, Sonnet Pasca... Published: 01 November 2016
Proceedings of 2nd International Electronic Conference on Medicinal Chemistry, doi: 10.3390/ecmc-2-b004
DOI See at publisher website ABS Show/hide abstract
Aromatic compounds (aminopurine, pyridine, quinoline, fluorene…) are excellent building blocks for the development of new drugs. Fluorenone and Fluorene containing natural products display diverse structural features due to their various ring junctions and chiral centers. Together with potential bioactivities, this family of natural products aroused considerable attention from synthetic chemists. They have interesting physicochemical properties and could be used as fluorescent probes1. They display also high therapeutic activities as anti-oxidant, anti-bacterial, anti-cancer, anti-malarial, anti-myocardial or anti-Alzheimer2-7. For example, Dendroflorin isolated from Dendrobium densiflorum, displays a high antioxidant activity. This compound is cytotoxic at 125.8 µg/mL and have an antimigratory effect at 1.0 µg/mL in 24h for H 460 cells (lungs cancer)3. Some 1,6-disubstituted fluorenones can also induce apoptosis and inhibited the tubulin polymerization in cells. They are active in the range of 0.15 to 0.29 µM for many cancer cells (T47D (breast), HCT 116 (colon), SNU 398 (carcinoma)) and represent thus interesting pharmacophore for the research of new anticancer drugs4. Isolated from the radix of Caulophyllum robustum Maxim, Caulophine has an anti-myocardial ischemia activity as a calcium antagonist5. Interestingly, some fluorenes have also shown a capacity to reduce the amyloid burden which induces severe neurodegeneration and cognitive deficits in Alzheimer’s disease6. Thus, fluorenes are attractive scaffolds for the design of new therapeutic agents. In our laboratory, we focus in the design and the preparation of novel asymmetric 2,7,9-trisusbtituted fluorenes. Herein, we describe the first steps of a convergent synthesis able to lead to a new library of fluorene enantiopurs with high potential bioactivities. References Kucherak O. A., Didier P., Mély Y., Klymchenko A. S., J. Phys. Chem. Lett. , 1, 2010, 616–620. Shi Y., Gao S., Tetrahedron 72, 2016, 1717-1735. Klongkumnuankarn P., Busaranon K., Chanvorachote P., Sritularak B., Jongbunpraset V., Likhitwitayawuid K., Hindawi Publishing Corporation, 2015, 1-10. Kemnitzer W., Sirisoma N., Jiang S., Kasibhatla S., Crogan-Grundy C., Tseng B., Drewe J., Xiong Cai S., Bioorg. & Med. Chem. Lett. 20, 2010, 1288-1292. Si K. W., Liu J. T., He L. C., Li X. K., Liu C. H. Li X. Q., Basic & Clinical Pharmacology & Toxicology, 107, 2010, 976-981. Hong H. S., Maezawa I., Budamagunta M., Rana S., Shi A., Vassar R., Liu R., Lam K. S., Cheng R. H., Hua D. H., Voss J. C., Jin L. W., Neurobiology of Aging 31, 2010, 1690-1699. Makanga M., Malaria Journal, 2014, 13:291.
Article 0 Reads 15 Citations Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(... Simone C.B. Gnoatto, Sophie Susplugas, Luciana Dalla Vechia,... Published: 01 January 2008
Bioorganic & Medicinal Chemistry, doi: 10.1016/j.bmc.2007.10.031
DOI See at publisher website PubMed View at PubMed
Article 0 Reads 1 Citation Type III collagen mimetic peptides designed with anti- or pro-aggregant activities on human platelets Viviane Pires, Julien Pecher, Sophie Da Nascimento, Pascal M... Published: 01 May 2007
European Journal of Medicinal Chemistry, doi: 10.1016/j.ejmech.2006.12.018
DOI See at publisher website PubMed View at PubMed
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