10.1007/BF00766381
The research aimed to investigate the synthesis and cardiotropic activity of stereoisomeric I-[2-(3,4-dimethoxyphenyl)ethyl]-2-methyl-4-ethynyl-4-acyloxy-trans-decahydroquinolines. The purpose was to study the new cardiotropic properties and the effect of the nature of the ester group on the pharmacological activity of these compounds. The researchers developed a method for obtaining acetate and benzoate esters based on individual isomers II and III and assessed their cardiovascular action. Key chemicals used in the synthesis process included acetylene alcohol isomers, AcCl, (EtCO)2O for acetate synthesis, and PhCOCI for benzoate synthesis, with methods A and B employed to optimize yield. The study concluded that the cardiotropic activity of the compounds was strongly dependent on the spatial orientation of the substituents attached to the C(4) atom, with different isomers exhibiting varying effects on mean arterial pressure (MAP) and heart contraction frequency (FHC). The research also suggested that the substances may undergo inactivation in the stomach, as oral administration did not show the same biological activity as intravenous administration.
10.1007/BF00479904
The research focuses on the synthesis of benzo[c]pyrilium salts with a cyclopolyether substituent and their conversion to isoquinoline derivatives. The key chemicals involved in the research include homoveratric acid and benzo-15-crown-5 as starting compounds. These compounds react in polyphosphoric acid to form ketone I. Carboxylic acid anhydrides, specifically acetic or propionic anhydride, along with perchloric acid, are used to convert ketone I into benzo[c]pyrilium perchlorates (IIa and IIb). Finally, ammonium carbamate is employed to transform these perchlorates into the desired isoquinoline derivatives (IIIa and IIIb). The study explores the potential of these compounds for developing new biologically active substances that can penetrate biological membranes or influence selective ion transfer in living organisms.
10.1016/j.bmcl.2011.06.037
The research focuses on the synthesis and evaluation of the anti-inflammatory potential of naturally occurring acetylated pseudoguaianolides, psilostachyin, and their analogues. The study involved the isolation of parthenin and coronopilin from Parthenium hysterophorus, followed by their semi-synthesis to produce various derivatives. The anti-inflammatory activity was assessed through the in vitro expression of TNF-α, IL-1β, and IL-6 in murine neutrophils. Reactants used in the synthesis included parthenin, coronopilin, acetic anhydride, propionic anhydride, butyric anhydride, and InCl3 as a catalyst, among others. Analytical techniques employed included X-ray crystallography for structural confirmation and flow cytometry for cytokine expression analysis. The experiments revealed that some analogues, particularly those without an α-methylene moiety, displayed improved anti-inflammatory activity compared to the parent molecules, indicating their potential as therapeutic agents.
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