32316-46-4Relevant academic research and scientific papers
Pyrazolyl-pyrimidones inhibit the function of human solute carrier protein SLC11A2 (hDMT1) by metal chelation
Embaby, Ahmed,Hediger, Matthias A.,Javor, Sacha,Manatschal, Cristina,Poirier, Marion,Reymond, Jean-Louis,Bühlmann, Sven,Pujol-Giménez, Jonai
supporting information, p. 1023 - 1031 (2020/10/06)
Solute carrier proteins (SLCs) control fluxes of ions and molecules across biological membranes and represent an emerging class of drug targets. SLC11A2 (hDMT1) mediates intestinal iron uptake and its inhibition might be used to treat iron overload diseases such as hereditary hemochromatosis. Here we report a micromolar (IC50 = 1.1 μM) pyrazolyl-pyrimidone inhibitor of radiolabeled iron uptake in hDMT1 overexpressing HEK293 cells acting by a non-competitive mechanism, which however does not affect the electrophysiological properties of the transporter. Isothermal titration calorimetry, competition with calcein, induced precipitation of radioactive iron and cross inhibition of the unrelated iron transporter SLC39A8 (hZIP8) indicate that inhibition is mediated by metal chelation. Mapping the chemical space of thousands of pyrazolo-pyrimidones and similar 2,2′-diazabiaryls in ChEMBL suggests that their reported activities might partly reflect metal chelation. Such metal chelating groups are not listed in pan-assay interference compounds (PAINS) but should be checked when addressing SLCs.
NEW BICYCLIC DIOXANES, THEIR PREPARATION AND THEIR USE AS FRAGRANT COMPOUNDS
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Page/Page column 10, (2011/02/24)
The invention is directed to the use of compounds of formula (I), as fragrant agents. In this formula: - R3 and R4 are independently a hydrogen atom, a C1-C6 alkyl group or a C2-C6 alkenyl group, R5 is a C1-C6 alkyl group, a C2-C6 alkenyl group or a (CH2)0-2-aryl group, R6 is a C1 -C6 alkyl group, a C2-C6 alkenyl group, a (CH2)0-2-aryl group or a C5- C6 cycloalkyl or cycloalkenyl group, and R7 is a hydrogen atom, a C1-C6 alkyl group or a C2-C6 alkenyl group; or R3, R4 and R5 are as above defined, and R6 and R7 together with the carbon atom to which they are attached form a C5-C6 cycloalkyl or cycloalkenyl group.
New bicyclic dioxanes, their preparation and their use as organoleptic compounds
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Page/Page column 9, (2011/04/14)
The present invention relates to novel 1,3-dioxane derivatives of formula (I) wherein each of R1 and R2 is a hydrogen atom, R3 and R4 are independently a hydrogen atom, a linear or branched C1-C6 alkyl group, or a linear or branched C2-C6 alkenyl group, and R5 is a linear or branched C1-C6 alkyl group, a linear or branched C2-C6 alkenyl group or a (CH2)0-2 - aryl group, and R6 and R7 are independently a hydrogen atom, a linear or branched C1-C6 alkyl group, a linear or branched C2-C6 alkenyl group or a (CH2)0-2 - aryl group, or R6 and R7 together with the carbon atom to which they are attached form a C5-C6 cycloalkyl group or a C5-C6 cycloalkenyl group, substituted or not; their preparation and their use as organoleptic compounds.
Highly selective room-temperature copper-catalyzed C-N coupling reactions
Shafir, Alexandr,Buchwald, Stephen L.
, p. 8742 - 8743 (2007/10/03)
Through the use of cyclic β-diketones as supporting ligands, the copper-catalyzed coupling of aryl iodides with aliphatic amines occurs at room temperature in as little as 1 h. These high reaction rates allow for the coupling of a wide range of aryl and heteroaryl iodides at room temperature. This method is highly tolerant of a number of reactive functional groups, including -Br and aromatic -NH2 as well as phenolic and aliphatic -OH. The high selectivity of the CuI-β-diketone catalyst for aliphatic amines represents a useful complement to the palladium-based methods. Copyright
TRIMETHYLSILYL TRIFLATE IN ORGANIC SYNTHESIS
Noyori, R.,Murata, S.,Suzuki, M.
, p. 3899 - 3910 (2007/10/02)
Trimethylsilyl triflate is a powerful silylating agent for organic compounds and acts as a catalyst which accelerates a variety of nucleophilic reactions in aprotic media.The reactions proceed via one-center, electrophilic coordination of the silyl group to hetero functional groups and exhibit unique selectivities.
