61190-10-1Relevant articles and documents
Synthesis and anti-parasitic activity of achiral N-benzylated phosphoramidic acid derivatives
Adeyemi, Christiana M.,Conibear, Anne C.,Hoppe, Heinrich C.,Isaacs, Michelle,Kaye, Perry T.,Klein, Rosalyn,Lobb, Kevin A.,Mnkandhla, Dumisani,Mutorwa, Marius K.,Nokalipa, Iviwe C.
, (2020/06/21)
Synthetic pathways have been developed to access a series of N-benzylated phosphoramidic acid derivatives as novel, achiral analogues of the established Plasmodium falciparum 1-deoxy-D-xylulose-5-phosphate reductase (PfDXR) enzyme inhibitor, FR900098. Bioassays of the targeted compounds and their synthetic precursors have revealed minimal antimalarial activity but encouraging anti-trypanosomal activity – in one case with an IC50 value of 5.4 μM against Trypanosoma brucei, the parasite responsible for Nagana (African cattle sleeping sickness). The results of relevant in silico modelling and docking studies undertaken in the design and evaluation of these compounds are discussed.
Novel inhibitor compounds specific of secreted non-pancreatic human a2phospholipase of group II
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Page/Page column 9, (2010/02/11)
The present invention relates to a compound of the following formula (I) and pharmaceutical compositions containing the compound of formula (I): wherein D, Y, A, B, p, q, W and R have the same meanings as defined in the specification.
A ONE-POT ISOQUINOLINE SYNTHESIS BY CYCLODEHYDROGENATION OF BENZYLAMINOACETALS WITH CHLOROSULFONIC ACID
Kido, Kazuko,Watanabe, Yasuo
, p. 1151 - 1154 (2007/10/02)
A direct preparation of the fully aromatized isoquinolines (3a-l) by the cyclodehydrogenation of benzylamnoacetals (2a-l) with chlorosulfonic acid is described.Comparing the behavior of chlorosulfonic acid with that of sulfuric acid toward 1,2-dihydroisoquinoline, it is able to be suggested that benzylaminoacetals were cyclized first to 1,2-dihydroisoquinolines, subsequently, dehydrogenated to the fully aromatized isoquinolines by the hydride abstraction with ClSO3H.Subtitution by a larger R3 group than isopropyl in the acetal ArCH(R3)NHCH2CH(OEt)2, interfered this second step, so the corresponding isoquinolines could not be obtained.