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作者:Gérald Guillaumet , Taner Dagcı ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2017, Vol.129, pp.41-52
摘要:Abstract(#br)Neurodegenerative disorders including Alzheimer's disease, Parkinson's disease, and Huntington's disease affect millions of people in the world. Thus several new approaches to treat brain disorders are under development. The aim of the present study is to synthe...
作者:... Güliz Armagan , Luciano Saso , Gérald Guillaumet
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2018, Vol.145, pp.113-123
摘要:Abstract(#br)Oxidative stress and apoptosis are both associated with various acute and chronic disorders. Thus, the aim of the present study is to synthesize imidazo[2,1- c ][1,2,4]triazines derivatives and to evaluate their effects in H 2 O 2 -induced oxidative stress in hu...
作者:... Franck Suzenet , Qi Sun , Gérald Guillaumet
来源:[J].Tetrahedron(IF 2.803), 2017, Vol.73 (37), pp.5485-5492
摘要:Abstract(#br)Ortho-chelation assistance was proved to be crucial for the success of the desulfitative Sonogashira cross-coupling reaction of thioamide-type pyridine derivatives and alkynes. Corresponding alkynylated products were obtained with moderate to excellent yields. Thanks...
作者:... Marie-Aude Hiebel , Gérald Guillaumet , Franck Suzenet
来源:[J].Tetrahedron Letters(IF 2.397), 2018
摘要:Abstract(#br)Magnesium in methanol was found to be an effective and inexpensive reagent for the dehalogenation of (hetero)aryl chlorides, bromides and iodides under mild conditions. The halogen/hydrogen exchange proceeded at room temperature and tolerated functional groups such a...
作者:... Jaime Rubio-Martínez , Gérald Guillaumet , M. Dolors Pujol
来源:[J].Tetrahedron(IF 2.803), 2015, Vol.71 (8), pp.1207-1214
摘要:Abstract(#br)A novel, general, and efficient one-pot sequential reaction toward a variety of 4-aminated-6-arylpyrrolo[2,3- d ]pyrimidines from 5-alkynylpyrimidines has been developed. Microwave-assisted metal-free intramolecular cyclization and amination provided moderate to exce...
作者:... Irina Zarafu , Vasile I. Parvulescu , Gérald Guillaumet
来源:[J].Tetrahedron Letters(IF 2.397), 2015, Vol.56 (39), pp.5349-5352
摘要:Abstract(#br)We describe herein the synthesis of 2-alkynylbenzoxazole and 2-alkynylbenzothiazole derivatives through the Sonogashira cross-coupling reaction of the corresponding thioethers and terminal alkynes under aerobic conditions, using CuI and Pd(dppf)Cl 2 as catalysts. The...
作者:... Agnès Chartier , Franck Suzenet , Gérald Guillaumet
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2016, Vol.109, pp.268-275
摘要:Abstract(#br)We report herein an efficient synthesis of 2-substituted furo[3,2- b ]pyridines and their biological evaluation as melatonin receptors ligands. The proposed eight-step sequence ending with a Suzuki coupling allowed a rapid access to various analogues. The steric hind...
作者:... Eric Pasquinet , Franck Suzenet , Gérald Guillaumet
来源:[J].Tetrahedron(IF 2.803), 2016, Vol.72 (10), pp.1337-1341
摘要:Abstract(#br)A modified approach to synthesize and isolate arylnitromethanes is described. The method takes advantage of the significant difference in acidity between the arylnitromethane and the major impurity of the reaction, the nitrite ester. The arylnitromethanes resulting f...
作者:... Mohamed Akssira , Gérald Guillaumet , Sylvain Routier
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2016, Vol.115, pp.311-325
摘要:Abstract(#br)An efficient synthetic strategy able to modulate the structure of the tetrahydropyridine isoindolone (Valmerin) skeleton was developed. A library of more than 30 novel final structures was generated. Biological activities on CDK5 and GSK3 as well as cellular effects ...
作者:... Richard Daniellou , Gérald Guillaumet , Mohamed Akssira
来源:[J].Tetrahedron Letters(IF 2.397), 2016, Vol.57 (24), pp.2591-2594
摘要:Abstract(#br)A series of novel 9α-substituted-13-(1,2,3-triazolo)-parthenolides 3 – 20 were efficiently synthesized and tested for their in vitro anticancer activity using the MTT colorimetric assay against four human cancer cell lines. 9α-Substituted-13-(1,2,3-triazolo)-par...

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