18305-96-9Relevant articles and documents
N-methylated diazabicyclo[3.2.2]nonane substituted triterpenoic acids are excellent, hyperbolic and selective inhibitors for butyrylcholinesterase
Heise, Niels,Friedrich, Sander,Temml, Veronika,Schuster, Daniela,Siewert, Bianka,Csuk, René
supporting information, (2021/11/08)
Triterpenoic acids (oleanolic, ursolic, betulinic, platanic and glycyrrhetinic acid) were acetylated and coupled with 1,3- or 1,4-diazabicyclo[3.2.2]nonanes to yield amides. Reaction of these amides with methyl iodide at the distal nitrogen of the bicyclic system gave the corresponding quaternary ammonium salts. These compounds were shown to act as excellent inhibitors of the enzyme butyrylcholinesterase (BChE) while being only weak inhibitors for acetylcholinesterase (AChE). Evaluation of the enzyme kinetics revealed these compounds to act as hyperbolic inhibitors for BChE while the results from molecular modeling gave an explanation for their selectivity between AChE and BChE.
Nitrogenous heterocyclic glycyrrhetinic acid derivatives, and preparation method and anti-influenza A virus application thereof
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Paragraph 0027-0028; 0071-0073, (2020/02/29)
The invention discloses nitrogenous heterocyclic glycyrrhetinic acid derivatives, and a preparation method and an anti-influenza A virus application thereof. The glycyrrhetinic acid derivatives comprise a nitrogen heterocyclic ring. A series of the glycyrrhetinic acid derivatives with anti-IAV activity are synthesized. The glycyrrhetinic acid derivatives have strong inhibitory activity on the influenza A virus (IAV), and have obviously stronger inhibitory activity on the influenza A virus than a common positive drug ribavirin, so that the glycyrrhetinic acid derivatives can be used for preparing anti-IAV drugs, and have no side effects.
Pentacyclic triterpenoid glycyrrhetinic acid derivative as well as preparation method and application thereof
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Paragraph 0046; 0051-0052, (2020/05/01)
The invention discloses a pentacyclic triterpenoid glycyrrhetinic acid derivative which has a structure as shown in a general formula 1 or a formula 7 in the specification, wherein each substituent isdefined in detail in the specification. The invention also discloses application of the pentacyclic triterpenoid glycyrrhetinic acid derivative in preparation of anti-HCV drugs. Huh7 cytotoxic activity results show that the pentacyclic triterpenoid glycyrrhetinic acid derivative is low in cytotoxicity and has research value. In-vitro anti-HCVcc result shows that glycyrrhetinic acid has relativelyweak anti-HCVcc activity, but the pentacyclic triterpenoid glycyrrhetinic acid derivative has relatively good anti-HCV activity.