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).
Lappaconitine derivative with analgesic activity, and preparation method and application thereof
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Paragraph 0387-0392, (2021/07/14)
The invention provides a lappaconitine derivative with analgesic activity, and a preparation method and application thereof. The structure of the lappaconitine derivative is as shown in formula I in the specification. The lappaconitine derivative provided by the invention is high in analgesic activity, good in water solubility and low in biotoxicity, can be used for preparing low-toxicity analgesic drugs, and is wide in application prospect.
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
