Bisbenzimidazoles as antimalarial agents

[0072]The following general procedures and intermediates were used to prepare the compounds described herein. Compounds for use in the present invention can be prepared as described in Scheme 1.

with n=0 to 10, and each R is independently selected from hydrogen, halogen, hydroxyl, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, alkylcarbonyloxy, formyl, alkylcarbonyl, alkyloxycarbonyl, halocarbonyl, haloalkyl, haloalkoxy, carbamoyl, cyano, nitro, sulfo, or a carboxyl group.

[0073]For example, each R is independently selected from H, —CO2H, Cl, F, Br, —OH, -Me, -Et, -nPr, -iPr, tBu, —OMe, —OEt, —OnPr, —OiPr, —OnBu, —OiBu, —OtBu, —O—C5—H11, —O—C6H13, —O—C7H15, —O—C8H17, —O—C9H19, —O—C10H21, —O—C11H23, O—C12H25, —O—C13H27, —O—C14H29, . . . , —OC18H37, . . . —OC24H49, —NH2, —NH(Me), —N(Me)2, —N(Et)2, —NH—CO-Me, —NH—CO-Et, —OCOMe, —OCOEt, —OCOnPr, —OCOiPr, —OCOnBu, —OCOiBu, —OCOtBu, —OCO—C5H11, —OCO—C6H13, —OCO—C7H15, —OCO—C8H17, —OCO—C9H19, —OCO—C10H21, —OCO—C11H23, OCO—C12H25, —OCO—C1