137766-76-8Relevant articles and documents
Biocatalytic Access to Piperazines from Diamines and Dicarbonyls
Borlinghaus, Niels,Gergel, Sebastian,Nestl, Bettina M.
, p. 3727 - 3732 (2018/04/14)
Given the widespread importance of piperazines as building blocks for the production of pharmaceuticals, an efficient and selective synthesis is highly desirable. Here we show the direct synthesis of piperazines from 1,2-dicarbonyl and 1,2-diamine substrates using the R-selective imine reductase from Myxococcus stipitatus as biocatalyst. Various N- and C-substituted piperazines with high activity and excellent enantioselectivity were obtained under mild reaction conditions reaching up to 8.1 g per liter.
Histone demethylase LSD1 (lysine specific demethylase 1) inhibitor
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Paragraph 0025, (2017/09/29)
The invention provides a histone demethylase LSD1 (lysine specific demethylase 1) inhibitor. The invention relates to piperazine-containing compounds and pharmacologically acceptable salts thereof and use of the piperazine-containing compounds and pharmacologically acceptable salts thereof as the LSD1 inhibitor; the general structural formula of the piperazine-containing compounds is described in the description. The invention belongs to the field of pharmaceutical chemistry. An in-vitro LSD1 activity inhibition test proves that the piperazine-containing compounds implemented by the invention have an obvious inhibiting effect for LSD1 activity, thus being used as active ingredients for preparing LSD1 inhibitor medicines.
Benzo[1,8]naphthyridine derivatives, their preparation and compositions containing them
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, (2008/06/13)
New benzo[b][1,8]naphthyridine derivatives of general formula (I), in which R1 is a hydrogen atom or a hydroxyl or alkyl radical, R2 is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkyloxy or alkylamino radical, R3 is a phenyl or phenylalkyl radical substituted with one or more halogen atoms or alkyl, cycloalkyl (3 to 6 C), alkyloxy, cyano, amino, alkylamino, dialkylamino, alkyloxyalkyl, hydroxyalkyl, hydroxyalkyloxy, methylenedioxy, aminoalkyl, alkylaminoalkyl or dialkylaminoalkyl radicals, or R3 is a heterocyclic radical, and R4 is a hydrogen atom or a fluorine atom, the alkyl radicals (1 to 4 C) being linear or branched, their salts, their preparation and compositions containing them. These new products are useful as antimicrobials, or in the treatment of AIDS. STR1