Council of Scientific and Industrial Research

Nicholas Piramal India Limited

Sunil Kumar Puri

Chandan Singh

Anil Kumar Dwivedi

Satyawan Singh

Ram Pratap

Sudhir Srivastava

Omkar Prasad Asthana

Ram Chandra Gupta

Jagdishwar Sahai Srivastava

Amiya Prasad Bhaduri

Harsh Pati Thapliyal

Guru Prasad Dutta

Pratima Srivastava

Vikash Chandra Pandey

Heetika Malik

Shio Kumar Singh

Swati Ajay Piramal

Francis Joseph Pinto

Chndan Singh

Pallvi Tiwari

The present invention relates to spiro 1,2,4-trioxanes of general formula 4. This invention more particularly relates to a process for the preparation of a series of spiro 1,2,4-trioxanes. Wherein, Ar represents aryl groups such as phenyl, 4-biphenyl, 4-chlorophenyl, 4-methoxyphenyl, 4-methylphenyl, 4-cyclohexylphenyl, 1-naphthyl, 2-naphthyl and the like and R represents hydrogen or the alkyl group such as methyl, ethyl and the like. Several of these compounds show high order of antimalarial activity against multidrug-resistant malaria in mice and thus hold promise as antimalarial agents against multidrug-resistant malaria.

Spiro-1,2,4-trioxanes

A combination kit for the treatment of malaria caused by() having individual doses of an anti-malarial agent, 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I) in the form of capsules; individual doses of the anti-malarial agent, chloroquine in the form of tablets; and instruction material for the administration of the two anti-malarial drugs. The combination kit is particularly suited for a 6 days treatment regimen where the treatment is rendered by five tablets containing 500 mg of chloroquine phosphate (equivalent to 300 mg base), three to be taken on day one and one each on days two and three; and five capsules containing 25 mg of 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I), one each to be taken on days two to six.

Combination kit used in the treatment of malaria

The present invention a novel use of primaquine derivative N-(3-ethylidinotetrahydrofuran-2-one)-N-(6-methoxy-8-quinolinyl)-1,4-pentanediamine in the treatment and controlling the spread of malaria. In particular, the present invention discloses a method of treatment of malaria by the use of primaquine derivative N-(3-ethylidinotetrahydrofuran-2-one)-N-(6-methoxy-8-quinolinyl)-1,4-pentanediamine as a gametocytocidal agent.

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The present invention relates to a novel series of antimalarial amino functionalized 1,2,4-trioxane analogues of formula 4 wherein Ar represents aryl groups such as phenyl, 4-biphenyl, 4-chlorophenyl, 4-methoxyphenyl, 4-methylphenyl and R represents phenyl, 4-methoxyphenyl, 4-chlorophenyl, 3,5-dichlorophenyl, 4-acetylaminophenyl, 1-naphthyl, 2-biphenyl, 4-biphenyl, 2-fluorene, 4-fluorophenyl, 2-trifluoromethylphenyl, 3-trifluoromethylphenyl and 4-trifluoromethylphenyl and the like.

Amino-functionalized 1,2,4-trioxanes useful as antimalarial agents and process for preparation thereof

Substituted 1,2,4-trioxanes useful as antimalarial agents and a process for the preparation thereof

The present invention relates to novel substituted 1,2,4-trioxanes that are useful as anti-malarial agents, and have a general formula 1,

Substituted 1,2,4-trioxanes as antimalarial agents and a process of producing the substituted 1,2,4-trioxanes

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Lucknow, India

Sunil Kumar Puri