FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2073172046> ?p ?o ?g. }

• W2073172046 endingPage "1042" @default.
• W2073172046 startingPage "1033" @default.
• W2073172046 abstract "Abstract A library of 52 pentamidine congeners in which the flexible pentyldioxy linker in pentamidine was replaced with various restricted linkers was tested for in-vitro activity against two Plasmodium falciparum strains and Leishmania donovani. The tested compounds were generally more effective against P. falciparum than L. donovani. The most active compounds against the chloroquine-sensitive (D6, Sierra Leone) and -resistant (W2, Indochina) strains of P. falciparum were bisbenzamidines linked with a 1,4-piperazinediyl or 1, 4-homopiperazinediyl moiety, with IC50 values (50% inhibitory concentration, inhibiting parasite growth by 50% in relation to drug-free control) as low as 7 nM based on the parasite lactate dehydrogenase assay. Seven piperazine-linked bisbenzamidines substituted at the amidinium nitrogens with a linear alkyl group of 3–6 carbons (22, 25, 27, 31) or cycloalkyl group of 4, 6 or 7 carbons (26, 32, 34) were more potent (IC50 &lt; 40 nM) than chloroquine or pentamidine as anti-plasmodial agents. The most active anti-leishmanial agents were 4,4′-[1,4-phenylenebis(methyleneoxy)]bisbenzenecarboximidamide (2, IC50 ∼ 0.290 μM) and 1,4-bis[4-(1H-benzimidazol-2-yl)phenyl] piperazine (44, IC50∼0.410 μM), which were 10- and 7-fold more potent than pentamidine (IC50 ∼ 2.90 μM). Several of the more active anti-plasmodial agents (e.g. 2,31, 33, 36–38) were also potent anti-leishmanial agents, indicating broad antiprotozoal properties. However, a number of analogues that showed potent anti-plasmodial activity (1, 18, 21, 22, 25–28, 32, 43, 45) were not significantly active against the Leishmania parasite. This indicates differential modes of anti-plasmodial and anti-leishmanial actions for this class of compounds. These compounds provide important structure-activity relationship data for the design of improved chemotherapeutic agents against parasitic infections." @default.
• W2073172046 created "2016-06-24" @default.
• W2073172046 creator A5003858499 @default.
• W2073172046 creator A5014644608 @default.
• W2073172046 creator A5028051807 @default.
• W2073172046 creator A5051860282 @default.
• W2073172046 creator A5058681890 @default.
• W2073172046 creator A5082120141 @default.
• W2073172046 date "2006-08-01" @default.
• W2073172046 modified "2023-10-03" @default.
• W2073172046 title "Anti-plasmodial and anti-leishmanial activity of conformationally restricted pentamidine congeners" @default.
• W2073172046 cites W1493318691 @default.
• W2073172046 cites W1968984252 @default.
• W2073172046 cites W1969918329 @default.
• W2073172046 cites W1972806542 @default.
• W2073172046 cites W1974387744 @default.
• W2073172046 cites W1981968564 @default.
• W2073172046 cites W1986640522 @default.
• W2073172046 cites W1986889483 @default.
• W2073172046 cites W1987626964 @default.
• W2073172046 cites W1992219001 @default.
• W2073172046 cites W1997545346 @default.
• W2073172046 cites W2001404273 @default.
• W2073172046 cites W2008962877 @default.
• W2073172046 cites W2009596876 @default.
• W2073172046 cites W2013880181 @default.
• W2073172046 cites W2023969818 @default.
• W2073172046 cites W2026277932 @default.
• W2073172046 cites W2032836303 @default.
• W2073172046 cites W2040170801 @default.
• W2073172046 cites W2043645060 @default.
• W2073172046 cites W2064262840 @default.
• W2073172046 cites W2067546715 @default.
• W2073172046 cites W2084889403 @default.
• W2073172046 cites W2098430714 @default.
• W2073172046 cites W2112614369 @default.
• W2073172046 cites W2113083913 @default.
• W2073172046 cites W2120153625 @default.
• W2073172046 cites W2133688074 @default.
• W2073172046 cites W2138909719 @default.
• W2073172046 cites W2140570882 @default.
• W2073172046 cites W2157739749 @default.
• W2073172046 cites W2168946125 @default.
• W2073172046 cites W2170048941 @default.
• W2073172046 cites W2179633317 @default.
• W2073172046 cites W21919429 @default.
• W2073172046 cites W2296263363 @default.
• W2073172046 doi "https://doi.org/10.1211/jpp.58.8.0003" @default.
• W2073172046 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16872549" @default.
• W2073172046 hasPublicationYear "2006" @default.
• W2073172046 type Work @default.
• W2073172046 sameAs 2073172046 @default.
• W2073172046 citedByCount "14" @default.
• W2073172046 countsByYear W20731720462013 @default.
• W2073172046 countsByYear W20731720462017 @default.
• W2073172046 countsByYear W20731720462020 @default.
• W2073172046 crossrefType "journal-article" @default.
• W2073172046 hasAuthorship W2073172046A5003858499 @default.
• W2073172046 hasAuthorship W2073172046A5014644608 @default.
• W2073172046 hasAuthorship W2073172046A5028051807 @default.
• W2073172046 hasAuthorship W2073172046A5051860282 @default.
• W2073172046 hasAuthorship W2073172046A5058681890 @default.
• W2073172046 hasAuthorship W2073172046A5082120141 @default.
• W2073172046 hasConcept C126322002 @default.
• W2073172046 hasConcept C185592680 @default.
• W2073172046 hasConcept C202751555 @default.
• W2073172046 hasConcept C203014093 @default.
• W2073172046 hasConcept C2776201271 @default.
• W2073172046 hasConcept C2776555147 @default.
• W2073172046 hasConcept C2776568683 @default.
• W2073172046 hasConcept C2776635100 @default.
• W2073172046 hasConcept C2777425658 @default.
• W2073172046 hasConcept C2777530519 @default.
• W2073172046 hasConcept C2777752497 @default.
• W2073172046 hasConcept C2777914695 @default.
• W2073172046 hasConcept C2778048844 @default.
• W2073172046 hasConcept C2778371730 @default.
• W2073172046 hasConcept C2778689377 @default.
• W2073172046 hasConcept C2781333301 @default.
• W2073172046 hasConcept C55493867 @default.
• W2073172046 hasConcept C71240020 @default.
• W2073172046 hasConcept C71924100 @default.
• W2073172046 hasConcept C86803240 @default.
• W2073172046 hasConcept C98274493 @default.
• W2073172046 hasConceptScore W2073172046C126322002 @default.
• W2073172046 hasConceptScore W2073172046C185592680 @default.
• W2073172046 hasConceptScore W2073172046C202751555 @default.
• W2073172046 hasConceptScore W2073172046C203014093 @default.
• W2073172046 hasConceptScore W2073172046C2776201271 @default.
• W2073172046 hasConceptScore W2073172046C2776555147 @default.
• W2073172046 hasConceptScore W2073172046C2776568683 @default.
• W2073172046 hasConceptScore W2073172046C2776635100 @default.
• W2073172046 hasConceptScore W2073172046C2777425658 @default.
• W2073172046 hasConceptScore W2073172046C2777530519 @default.
• W2073172046 hasConceptScore W2073172046C2777752497 @default.
• W2073172046 hasConceptScore W2073172046C2777914695 @default.
• W2073172046 hasConceptScore W2073172046C2778048844 @default.
• W2073172046 hasConceptScore W2073172046C2778371730 @default.

• next