Description
DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of
T. brucei N-myristoyltransferase (T
bNMT) with an apparent K
i value of 1.44 nM.
T. brucei is the parasite responsible for human African trypanosomiasis (HAT), also known as African sleeping sickness, and is transmitted through the tsetse fly. DDD85646 administration in mice (12.5 mg/kg for four days) ameliorated
T. brucei in an acute mouse model of HAT. It less potently inhibits growth of
T. cruzi (EC
50 = 6.9 μM).
