US Government As Represented by the Secretary of the Army

Lucia Gerena

John P Scovill

Dennis E Kyle

Kevin K Pitzer

Compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo [2,1-b]quinazoline-6,12-dione compounds of Formula I. wherein A, B, C, D, B, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, with the proviso that not more than three of A, B, C, D, E, F, G and H are other than carbon; wherein Rthrough Rare independently selected from the group consisting of, but not limited to H, the halogens (F, Cl, Br, and I), alkyl groups, trifluoromethyl groups, methoxyl groups, the carboxy methyl or carboxy ethyl group (COOCHor COOCHCH), nitro, aryl, heteroaryl, cyano, amino, dialkylaminoalkyl, 1-(4-alkylpiperazinyl), and the pharmaceutically acceptable salts thereof; and wherein X is independently selected from the group consisting of any atom especially oxygen, or any side chain necessary to make the indolo[2,1-b]quinazoline-6,12-dione compound a 'prodrug' as the term is understood by one of ordinary skill in the art of medicinal chemistry. In other words, a side chain having a structure where a carbon-nitrogen double bond bears substituents that make the prodrug more water soluble and bioavailable.

Indolo[2,1-b] quinazole-6,12-dione antimalarial compounds and methods of treating malaria therewith

Indolo&lsqb;2,1-b&rsqb; quinazole-6, 12-dione antimalarial compounds and methods of treating malaria therewith

Compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo&lsqb;2,1-b&rsqb;quinazoline-6,12-dione compounds of Formula I.

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Silver Spring, MD, United States of America

Lucia Gerena