NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection . NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC 50 0 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC 50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19 , respectively.
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