1,3-dihydro-1-hydroxy-2,1-Benzoxaborole-7-propanoic acid

AN3661 is active at nanomolar (IC ₅₀ =20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC ₅₀ =64 nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC ₅₀ 60.5 μM against Jurkat cells, and all other CC ₅₀ values greater than the highest concentrations tested (25 μM or above).
AN3661 inhibits the stability of P. falciparum transcripts.

AN3661 (50-200 mg.kg; po; daily for 4 days) inhibits murine P. berghei infections with ED ₉₀ (4 days) 0.34 mg/kg.
AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED ₉₀ 4 days after initiation of treatment is 0.57 mg/kg.