US Government As Represented by the Secretary of the Army

Other

John P Scovill

Daniel L Klayman

T Scott Griffin

Carl J Mason

Joseph F Bartosevich

Dennis E Kyle

Kevin K Pitzer

Lucia Gerena

Arthur S Dobek

Norman E Morrison

Armando Gonzalez

Steven D Grant

Samuel P Massie

Charles F Franchino

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.

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

This invention relates to various 2-acetyl- and 2-propionylpyridine thiosemicarbazones which are substituted on the 4-nitrogen atom. These compounds are useful in the treatment of gonorrhea and, in addition, many are useful either in the treatment of malaria or bacterial infection. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones.

2-acetyl-and 2-propionylpyridine thiosemicarbazones

This invention relates to novel 2-acetyl- and 2-propionylpyridine selenosemicarbazones. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the selenosemicarbazones.

2-acetyl- and 2-propionylpyridine selenosemicarbazones

This invention relates to novel transition metal complexes of 2-acetyl- and -propionylpyridine thiosemicarbazones, their selenium analogs. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones and their selenium analogs.

Transition metal complexes of the selenium analogs of 2-acetyl- and

Medicinal 2-acetyl- and 2-propionylpyridine thiosemicarbazones and

Method for treating bacterial infections with 2-acetyl- and

This invention relates to the preparation and use of various 2-acetyl quiine thiosemicarbazones which are substituted on the 4-nitrogen atom. These compounds are useful in the treatment of gonorrhea and, in addition, many are useful either in the treatment of malaria or bacterial infections, such as leprosy and meningitis.

2-Acetyl quinoline thiosemicarbazones useful in treatment of gonorrhea,

This invention relates to various 2-acetyl- and 2-propionylpyridine thioscarbazones which are substituted on the 4-nitrogen atom. These compounds are useful in the treatment of gonorrhea and, in addition, many are useful either in the treatment of malaria or bacterial infection. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones.

Method for treating gonorrhea infections with 2-acetyl- and

2-Acetyl-and 2-propionylpyridine thiosemicarbazones as antimalarials

2-Acetyl-and 2-propionylpyridine thiosemicarbazones

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Rockville, MD, United States of America

John P Scovill