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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
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,
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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