75335-16-9Relevant 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.
Assessment of antiplatelet activity of 2-aminopyrimidines
Giridhar, Rajani,Tamboli, Riyaj S.,Ramajayam,Prajapati, Dhaval G.,Yadav
, p. 428 - 432 (2012/07/03)
A series of 4,6-diaryl-2-aminopyrimidines was developed as antiplatelet agents and their potency was evaluated by in vitro assay. Compound 14k was found to be two times more potent than aspirin. These encouraging results could be helpful for the development of new antiplatelet compounds.
One pot synthesis of 1-(2-hydroxyphenyl)-3-phenylpropane-1,3-diones by modified Baker-Venkataraman transformation using microwave irradiation
Lamba,Kumar, Suresh,Makrandi
, p. 133 - 134 (2007/10/03)
Reaction of 2-hydroxyacetophenones with aromatic acid anhydrides in the presence of anhydrous barium hydroxide in dimethyl sulfoxide using microwave irradiation gives 1-(2-hydroxyphenyl)-3-phenylpropane-1,3-diones directly in a single pot reaction in high yields.
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors
Costantino, Luca,Rastelli, Giulio,Gamberini, Maria Cristina,Vinson, Joe A.,Bose, Pratima,Iannone, Anna,Staffieri, Mariagrazia,Antolini, Luciano,Del Corso, Antonella,Mura, Umberto,Albasini, Albano
, p. 1881 - 1893 (2007/10/03)
Starting from the inhibitory activity of the flavonoid Quercetin, a series of 4H-1-benzopyran-4-one derivatives was synthesized and tested for inhibition of aldose reductase, an enzyme involved in the appearance of diabetic complications. Some of the compounds obtained display inhibitory activity similar to that of Sorbinil but are more selective than Quercetin and Sorbinil with respect to the closely related enzyme, aldehyde reductase, and also possess antioxidant activity. Remarkably, these compounds possess higher pK(a) values than carboxylic acids, a characteristic which could make the pharmacokinetics of these compounds very interesting. Molecular modeling investigations on the structures of inhibitors bound at the active site of aldose reductase were performed in order to suggest how these new inhibitors might bind to the enzyme and also to interpret structure-activity relationships.
New synthesis of 1,3-diarylpropane-1,3-diones
Bansal,Singh,Khanna
, p. 586 - 587 (2007/10/03)
1,3-Diarylpropane-1,3-diones have been synthesized by (i) UV irradiation and thermal rearrangement of o-aroyloxyacetophenones and (ii) microwave irradiation of aroyl chlorides and o-hydroyacetophenones.
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.
