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. 2019 Jul 18;4(3):108. doi: 10.3390/tropicalmed4030108

Table 7.

Advanced novel small molecules optimized for antiwolbachial efficacy.

AWZ1066S [86] CBR490 [92] CBR417 [92]
Series azaquinazoline quinazoline (methylpyridine) quinazoline (oxadiazole)
Structure graphic file with name tropicalmed-04-00108-i004.jpg graphic file with name tropicalmed-04-00108-i005.jpg graphic file with name tropicalmed-04-00108-i006.jpg
Activity C6/36 EC50 = 2.5 nM;
microfilariae EC50 = 121 nM; 		LDW1 EC50 = 33 nM;
B. pahangi ovaries ex vivo EC50 < 111 nM		 LDW1 EC50 = 24 nM;
B. pahangi ovaries ex vivo EC50 = 356 nM
Efficacy >99% wLS depletion in adult female L. sigmodontis: 50 mg/kg bid 7 days
>90% wBm depletion in adult female B. malayi: 100 mg/kg bid 7 days		 >99% wLS depletion in adult female L. sigmodontis:
200 mg/kg SINGLE DOSE, or
100 mg/kg one dose given per week ×2, or 30 mg/kg qd (quaque die, once a day) for 7 days		 >99% wLS depletion in adult female L. sigmodontis:
200 mg/kg SINGLE DOSE, or
100 mg/kg one dose given per week x2, or 60 mg/kg qd for 4 days