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编 号:F748147
分子式:C30H32N8O4
分子量:568.63
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生物活性:
S-MGB-234 is a minor groove binder of Animal African Trypanosomiasis (AAT). S-MGB-234 displays excellent in vitro activities against the principal causative organisms of AAT; Trypanosoma congolense, and Trypanosoma vivax. S-MGB-234 does not show cross-resistance with the current diamidine agents and are not internalized via the transporters used by diamidines.

体内研究:
S-MGB-234 (compound 7) provides total cure and no relapses in mice (cured/infected, 4/4), when treated with 2 applications of 50 mg/kg i.p.. Partial cure (1/4) is seen in mice treated with four daily applications of 10 mg/kg i.p., whilst only two applications of S-MGB-234 (compound 7) at 10 mg/kg i.p. gives no cure but prolongs survival relative to the untreated control.

体外研究:
S-MGB-234 (compound 7) (69 hours) shows nontoxic to L6 cells with an EC50 of 20.39 μM.
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