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Istituto di scienza dell'alimentazione

Torna all'elenco Contributi in rivista anno 2002

Contributo in rivista

Tipo: Articolo in rivista

Titolo: Mixed steroidal 1,2,4,5-tetraoxanes: antimalarial and antimycobacterial activity

Anno di pubblicazione: 2002

Autori: Solaja BA, Terzic N, Pocsfalvi G, Gerena L, Tinant B, Opsenica D, Milhous WK.

Affiliazioni autori: B. A. Šolaja, N. Terzić, G. Pocsfalvi, L. Gerena, B. Tinant, D. Opsenica, W. K. Milhous Faculty of Chemistry, University of Belgrade, Yugoslavia, Istituto di Scienze dell'Alimentazione, CNR Avellino, Italy, Institute of Chemistry, Technology and Metallurgy, Belgrade, Yugoslavia, Laboratoire de Chimie Physique et de Cristallographie, Université Catholique de Louvain, Belgium, Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington

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Abstract: Mixed 1,2,4,5-tetraoxanes possessing simple spirocycloalkane and spirocholic acid-derived substituents were prepared and shown to have significantly higher in vitro antimalarial activity than bis-substituted tetraoxanes. Out of 41 synthesized tetraoxanes, 12 were in vitro more potent against Plasmodium falciparum chloroquine-resistant W2 clone than artemisinin, and the most potent one was 2.4 times as active as arteether. In addition, 9 compounds exhibit higher activity than chloroquine against P. falciparum chloroquine-susceptible D6 clone. Cytotoxicity was assessed for most active compounds against the Vero cell line, showing a cytotoxicity/antimalarial potency ratio of 1/(1400-9500). For the first time, tetraoxanes were screened against Mycobacterium tuberculosis with MICs as low as 4.73 microM against H37Rv strain. Mixed tetraoxanes were synthesized in a simple procedure from cholic acid methyl esters by direct coupling of steroidal gem-dihydroperoxide to simple ketones and further transformed into corresponding acids and amides.

Pagine da: 3331

Pagine a: 3336


Journal of medicinal chemistry American Chemical Society,
Paese di pubblicazione: Stati Uniti d'America
Lingua: inglese
ISSN: 0022-2623

Numero volume: 45

Altre informazioni: Brevetto internazionale: MIXED STEROIDAL 1,2,4,5-TETRAOXANE COMPOUNDS AND METHOD OF MAKING AND USING THEREOF, International application number: WO 03/068736 A2; Brevetto USA: MIXED STEROIDAL 1,2,4,5-TETRAOXANE COMPOUNDS AND METHOD OF MAKING AND USING THEREOF, “United States Patent Application Publication” Pub. No. US 2004/0019200 A1, pub date: jan.29, 2004

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