654676-92-3Relevant academic research and scientific papers
Functionalization of Alkynes and Alkenes Using a Cascade Reaction Approach: Synthesis of β-Keto Sulfones under Metal-free Conditions
Kumar, Mukesh,Ahmed, Riyaz,Singh, Maninder,Sharma, Shweta,Thatikonda, Thanusha,Singh, Parvinder Pal
, p. 716 - 725 (2020/01/22)
Here, we are reporting a multicomponent cascade reaction approach for the synthesis of β-keto sulfones by exploiting differential reactivity pattern of substrates under open-atmosphere and metal-free conditions. The coupling partners are aryldiazonium salts, unsaturated compounds, and DABSO. The optimized conditions worked well with both alkenes and alkynes. Moreover, the reaction also works with metabisulfite for the source of sulfone. The controlled liquid chromatography-mass spectrometry and 18O-labelled experiments suggested that air is a source of the incoming oxygen atom of the keto group of β-keto sulfones.
Synthesis and evaluation of monoamidoxime derivatives: Toward new antileishmanial compounds
Paloque, Lucie,Bouhlel, Ahlem,Curti, Christophe,Dumtre, Aurélien,Verhaeghe, Pierre,Azas, Nadine,Vanelle, Patrice
supporting information; experimental part, p. 2984 - 2991 (2011/07/08)
A new series of monoamidoxime derivatives was synthesized using manganese(III) acetate by microwave irradiation. Several amidoximes (27-31, 33, 38) showed valuable in vitro activities toward Leishmania donovani promastigotes, exhibiting IC50 values between 5.21 and 7.89 μM. In parallel, the cytotoxicity of these compounds was evaluated on murine J774A.1 cells, revealing the corresponding selectivity index (SI). Among the 13 tested compounds, 4 monoamidoximes (27-30) exhibited an SI more than 20 times better than pentamidine. Moreover, monoamidoxime 28 (4-[5-Benzyl-3-(4- fluorophenylsulfonyl)-5-methyl-4,5-dihydrofuran-2-yl]-N′- hydroxybenzimidamide) is 40 times more selective than pentamidine, and 1.6 times more than amphotericin B, used as reference drug compounds.
Synthesis and evaluation of original amidoximes as antileishmanial agents
Bouhlel, Ahlem,Curti, Christophe,Dumtre, Aurélien,Laget, Michle,Crozet, Maxime D.,Azas, Nadine,Vanelle, Patrice
experimental part, p. 7310 - 7320 (2010/11/17)
An original series of amidoxime derivatives was synthesized using manganese(III) acetate, Buchwald-Hartwig and Heck reactions. Two amidoximes (39 and 52) showed interesting in vitro activities toward Leishmania donovani promastigotes, exhibiting 8.3 and 8.8 μM IC50 values. Moreover, the cytotoxicity of these compounds was evaluated on human THP1 cells, giving access to the corresponding selectivity index. Among the 25 tested compounds, amidoximes 38 and 39 and diamidoximes 50 and 52 exhibited a better selectivity index than pentamidine used as a drug compound reference.
CHEMICAL COMPOUNDS
-
Page 103, (2010/02/06)
Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described
