1711-11-1Relevant articles and documents
Structure-activity evaluation of new uracil-based non-nucleoside inhibitors of HIV reverse transcriptase
Matyugina, Elena S.,Valuev-Elliston, Vladimir T.,Geisman, Alexander N.,Novikov, Mikhail S.,Chizhov, Alexander O.,Kochetkov, Sergey N.,Seley-Radtke, Katherine L.,Khandazhinskaya, Anastasia L.
, p. 1443 - 1451 (2013)
A new series of potential nonnucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs) based on the carbocyclic 5′-nor-uracil scaffold were designed and synthesized. Three different aspects of the scaffold were investigated: the effects of adding a linker between the carbocyclic and phenyl fragments, introduction of different substituents on the benzoyl residue and replacing the central carbocyclic ring with a benzyl group. Analogues of 2′,3′-dideoxy-2′,3′-didehydro-5′-nor-uridine, bearing 3,5-dichloro- or 3,5-dimethylbenzoyl groups, showed inhibitory activity against HIV-RT wild-type (IC50 5-10 μM) and mutants L100I (IC 50 1.2-2.1 μM) and K103N (IC50 8-17 μM).
Direct Synthesis of Enamides via Electrophilic Activation of Amides
Berger, Martin,Kaiser, Daniel,Maulide, Nuno,Spie?, Philipp
supporting information, p. 10524 - 10529 (2021/07/28)
A novel, one-step N-dehydrogenation of amides to enamides is reported. This reaction employs the unlikely combination of LiHMDS and triflic anhydride, which serves as both the electrophilic activator and the oxidant, and is characterized by its simple setup and broad substrate scope. The synthetic utility of the formed enamides was readily demonstrated in a range of downstream transformations.
TOPICAL PHOSPHOINOSITIDE 3-KINASE INHIBITORS
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Paragraph 0485; 0486, (2020/08/20)
The present invention provides compounds and topical formulations including the compounds for the treatment of vascular malformations, wherein the compounds are according to formula (I): wherein subscript m, L1, R1, and L1
