76937-63-8Relevant academic research and scientific papers
Synthesis of novel 4,6-diaryl-2-aminopyrimidines as potential antiplasmodial agents
Giridhar, Rajani,Tamboli, Riyaj S.,Prajapati, Dhaval G.,Soni, Sanket,Gupta, Sarita,Yadav
, p. 3309 - 3315 (2013/07/27)
A novel series of 4,6-diaryl-2-aminopyrimidines 8a-o has been synthesized and evaluated for in vitro antiplasmodial activity against Plasmodium falciparum. Out of the 15 compounds synthesized and tested, 6 compounds have shown IC50 values in the range of 1.61-9.53 μg/mL. These compounds are several times more potent than chloroquine and quinine, the two standard drugs used for the purpose of comparison.
BIOSYNTHESIS OF A RETROCHALCONE ECHINATIN: INVOLVEMENT OF O-METHYLTRANSFERASE TO LICODIONE
Ayabe, Shin-Ichi,Yoshikawa, Takafumi,Kobayashi, Miyuki,Furuya, Tsutumo
, p. 2331 - 2336 (2007/10/02)
In order to clarify the O-methylation step in the bisynthesis of a retrochalcone, echinatin (4,4'-dihydroxy-2-methoxychalcone), methyl transfer from S-adenosyl-L-methionine (SAM) to licodione (1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)-1,3-propanedione) in the cell-free extract of the cultured cells of Glycyrrhiza echinata was examined.Time course of methyl transferring activity during culture cycle in 4 strains was correlated to echinatin content.The enzyme catalysing this reaction, licodione O-methyltransferase (LMT), was purified 135-fold.Substrate specificity studies implied that the hydroxy group ortho to the C3 linkage in licodione was methylated in this reaction.O-Methyl-licodiones were synthesized for comparison and the sole product of LMT-catalysed reaction was identified as 2'-O-methyl-licodione.A possible scheme for the last steps of echinatin biosynthesis is proposed. - Key Word Index: Glycyrrhiza echinata; Leguminosae; cell culture; cell free extract; retrochalcone biosynthesis; enzyme; O-methyltransferase; echinatin; licodione; O-methyl-licodiones.
