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A series of 21 compounds of trisubstituted pyrimidine derivatives have been synthesized and evaluated for their in vitro topoisomerase II inhibitory activity against filarial parasite
Setaria cervi. Out of these, five compounds (
12,
13,
14,
25 and
28) exhibited 70–80% inhibition at 10
μg/mL and three compounds (
13,
14 and
28) have shown 40–60% inhibition at 5
μg/mL concentration.
A series of 21 compounds of trisubstituted pyrimidine derivatives have been synthesized and evaluated for their in vitro topoisomerase II inhibitory activity against filarial parasite
Setaria cervi. Out of these, seven compounds (
8,
11–
14,
25 and
28) have shown 60–80% inhibition at 40 and 20
μg/mL concentration. Five compounds (
12,
13,
14,
25 and
28) exhibited 70–80% inhibition at 10
μg/mL concentration and three compounds (
13,
14 and
28) have shown 40–60% inhibition at 5
μg/mL concentration. All the above mentioned compounds have shown better topo II inhibitory activity than standard antifilarial drug (DEC) and enzyme topo II inhibitors (Novobiocin, Nalidixic acid).