Diversity-oriented synthesis and activity evaluation of substituted bicyclic lactams as anti-malarial against Plasmodium falciparum.
Citations
56 citations
27 citations
18 citations
14 citations
5 citations
References
168 citations
"Diversity-oriented synthesis and ac..." refers background in this paper
...Biologically active lactams range from β-lactams, used in diverse therapeutic areas viz serine-dependent enzyme inhibitors, matrix-metalloprotease inhibitors, and even apoptosis inductors [22,23], the inhibition of HIV-1 protease, antitumor activity, anti-malarial activity, and cholesterol absorption inhibition [24-30], peptides, bicyclic lactams (as potential anticancer and anti-malarials) etc....
[...]
136 citations
"Diversity-oriented synthesis and ac..." refers methods in this paper
...Compound D exhibited the 77.84 and 79.34% of inhibition in drug-sensitive clones 3D7 and HB3, respectively, whereas 59.3% in drug-resistant clone Dd2 at 50 μM of concentration (Figure 3A,B)....
[...]
...Plasmodium falciparum clones used in this study 3D7, Dd2 and HB3 [12-14], were cultured in O+ human erythrocytes supplemented with RPMI 1640 (Invitrogen, USA) 24 mM sodium bicarbonate (Sigma, USA), 0.1 mM hypoxanthine (Invitrogen, USA), 25 mg/ml gentamicin (Invitrogen, USA) and 0.5% AlbuMax I (Invitrogen, USA), according to methods described earlier [15]....
[...]
...Upon testing this focused library for their anti-malarial activity, dinitro/diamine substituted bicyclic lactams were found most effective growth inhibitory compound against both drug-resistant clone Dd2 and drug-sensitive clones HB3 and 3D7 of P. falciparum....
[...]
...Compound C exhibited the 48.6 and 39.9% of inhibition in drug-sensitive clones HB3 and 3D7, respectively, whereas 34.24% in drug-resistant clone Dd2 at 10 μM of concentration; also at 50 μM of concentration, it showed 85.27 and 88.35% of inhibition in drug-sensitive clones 3D7 and HB3, respectively, whereas 67.27% in drugresistant clone Dd2....
[...]
...(A) Bar graph showing the growth-inhibitory effect of dintro-substituted compound C at 50 μM concentration on sorbitol synchronized P. falciparum drug-sensitive clones 3D7, HB3 and drug-resistant clones Dd2....
[...]
134 citations
"Diversity-oriented synthesis and ac..." refers background in this paper
...Biologically active lactams range from β-lactams, used in diverse therapeutic areas viz serine-dependent enzyme inhibitors, matrix-metalloprotease inhibitors, and even apoptosis inductors [22,23], the inhibition of HIV-1 protease, antitumor activity, anti-malarial activity, and cholesterol absorption inhibition [24-30], peptides, bicyclic lactams (as potential anticancer and anti-malarials) etc....
[...]
122 citations
"Diversity-oriented synthesis and ac..." refers background in this paper
...Of the nearly 1,400 drugs registered worldwide in the last quarter of the 20th Century, only four were anti-malarials [3]....
[...]