Приказ основних података о документу
Mixed steroidal 1,2,4,5-tetraoxanes: Antimalarial and antimycobacterial activity
dc.creator | Šolaja, Bogdan | |
dc.creator | Terzić, Nataša | |
dc.creator | Pocsfalvi, Gabriella | |
dc.creator | Gerena, L. | |
dc.creator | Tinant, Bernard | |
dc.creator | Opsenica, Dejan | |
dc.creator | Milhous, Wilbur K. | |
dc.date.accessioned | 2019-01-30T17:10:47Z | |
dc.date.available | 2019-01-30T17:10:47Z | |
dc.date.issued | 2002 | |
dc.identifier.issn | 0022-2623 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/91 | |
dc.description.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 μM 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. | en |
dc.publisher | American Chemical Society (ACS) | |
dc.rights | restrictedAccess | |
dc.source | Journal of Medicinal Chemistry | |
dc.title | Mixed steroidal 1,2,4,5-tetraoxanes: Antimalarial and antimycobacterial activity | en |
dc.type | article | |
dc.rights.license | ARR | |
dc.citation.volume | 45 | |
dc.citation.issue | 16 | |
dc.citation.spage | 3331 | |
dc.citation.epage | 3336 | |
dc.citation.other | 45(16): 3331-3336 | |
dc.citation.rank | M21 | |
dc.identifier.pmid | 12139444 | |
dc.identifier.doi | 10.1021/jm020891g | |
dc.identifier.scopus | 2-s2.0-0036682037 | |
dc.identifier.wos | 000177142800002 | |
dc.type.version | publishedVersion |