FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3009107412> ?p ?o ?g. }

• W3009107412 endingPage "131088" @default.
• W3009107412 startingPage "131088" @default.
• W3009107412 abstract "We describe the enantioselective synthesis and biological evaluation of 4-(2-amino-1-hydroxyethyl)pyridines (4 AHPs) as new antimalarial drug candidates. In particular, two routes to obtain the key-intermediate 4-vinyl-pyridine were studied. These routes are based on a Kröhnke-type cyclization or on metal-catalyzed reactions. The Kröhnke-type cyclization route is faster but only efficient at low scale since this pathway involves a Wittig reaction that requires severe temperature-control. Consequently, we designed a second route based on metal-catalyzed reactions. This way is longer but the 4-vinyl-pyridine can be obtained on a 5 g scale at least. Finally, a regioselective SN2 ring-opening of enantiopure epoxides by alkyl primary amines allowed the synthesis of eight 4-AHPs with global yields up to 41%. These compounds show strong in vitro antimalarial activity against P. falciparum strains and are more active that chloroquine and mefloquine. These results demonstrate that 4-AHPs are promising antimalarial drug candidates." @default.
• W3009107412 created "2020-03-13" @default.
• W3009107412 creator A5006338056 @default.
• W3009107412 creator A5009647802 @default.
• W3009107412 creator A5011848079 @default.
• W3009107412 creator A5028441333 @default.
• W3009107412 creator A5040892203 @default.
• W3009107412 creator A5051134428 @default.
• W3009107412 creator A5060029531 @default.
• W3009107412 creator A5061635410 @default.
• W3009107412 date "2020-04-01" @default.
• W3009107412 modified "2023-10-14" @default.
• W3009107412 title "Enantiopure substituted pyridines as promising antimalarial drug candidates" @default.
• W3009107412 cites W1970173074 @default.
• W3009107412 cites W1974192933 @default.
• W3009107412 cites W1974376328 @default.
• W3009107412 cites W1983040571 @default.
• W3009107412 cites W1983988243 @default.
• W3009107412 cites W1994403933 @default.
• W3009107412 cites W1994741969 @default.
• W3009107412 cites W2000627032 @default.
• W3009107412 cites W2015145161 @default.
• W3009107412 cites W2018191599 @default.
• W3009107412 cites W2020101417 @default.
• W3009107412 cites W2027560783 @default.
• W3009107412 cites W2038674755 @default.
• W3009107412 cites W2059814420 @default.
• W3009107412 cites W2061104972 @default.
• W3009107412 cites W2092207998 @default.
• W3009107412 cites W2093959602 @default.
• W3009107412 cites W2100441435 @default.
• W3009107412 cites W2105668259 @default.
• W3009107412 cites W2114971505 @default.
• W3009107412 cites W2131232496 @default.
• W3009107412 cites W2142352308 @default.
• W3009107412 cites W2148462128 @default.
• W3009107412 cites W2158015870 @default.
• W3009107412 cites W2185452549 @default.
• W3009107412 cites W2335289071 @default.
• W3009107412 cites W2738277744 @default.
• W3009107412 doi "https://doi.org/10.1016/j.tet.2020.131088" @default.
• W3009107412 hasPublicationYear "2020" @default.
• W3009107412 type Work @default.
• W3009107412 sameAs 3009107412 @default.
• W3009107412 citedByCount "6" @default.
• W3009107412 countsByYear W30091074122021 @default.
• W3009107412 countsByYear W30091074122022 @default.
• W3009107412 countsByYear W30091074122023 @default.
• W3009107412 crossrefType "journal-article" @default.
• W3009107412 hasAuthorship W3009107412A5006338056 @default.
• W3009107412 hasAuthorship W3009107412A5009647802 @default.
• W3009107412 hasAuthorship W3009107412A5011848079 @default.
• W3009107412 hasAuthorship W3009107412A5028441333 @default.
• W3009107412 hasAuthorship W3009107412A5040892203 @default.
• W3009107412 hasAuthorship W3009107412A5051134428 @default.
• W3009107412 hasAuthorship W3009107412A5060029531 @default.
• W3009107412 hasAuthorship W3009107412A5061635410 @default.
• W3009107412 hasBestOaLocation W30091074121 @default.
• W3009107412 hasConcept C146686406 @default.
• W3009107412 hasConcept C161790260 @default.
• W3009107412 hasConcept C178790620 @default.
• W3009107412 hasConcept C185592680 @default.
• W3009107412 hasConcept C203014093 @default.
• W3009107412 hasConcept C21951064 @default.
• W3009107412 hasConcept C2777199930 @default.
• W3009107412 hasConcept C2778048844 @default.
• W3009107412 hasConcept C2778371730 @default.
• W3009107412 hasConcept C2779485729 @default.
• W3009107412 hasConcept C59759590 @default.
• W3009107412 hasConcept C60002323 @default.
• W3009107412 hasConcept C71240020 @default.
• W3009107412 hasConcept C86803240 @default.
• W3009107412 hasConcept C93237805 @default.
• W3009107412 hasConcept C96765332 @default.
• W3009107412 hasConceptScore W3009107412C146686406 @default.
• W3009107412 hasConceptScore W3009107412C161790260 @default.
• W3009107412 hasConceptScore W3009107412C178790620 @default.
• W3009107412 hasConceptScore W3009107412C185592680 @default.
• W3009107412 hasConceptScore W3009107412C203014093 @default.
• W3009107412 hasConceptScore W3009107412C21951064 @default.
• W3009107412 hasConceptScore W3009107412C2777199930 @default.
• W3009107412 hasConceptScore W3009107412C2778048844 @default.
• W3009107412 hasConceptScore W3009107412C2778371730 @default.
• W3009107412 hasConceptScore W3009107412C2779485729 @default.
• W3009107412 hasConceptScore W3009107412C59759590 @default.
• W3009107412 hasConceptScore W3009107412C60002323 @default.
• W3009107412 hasConceptScore W3009107412C71240020 @default.
• W3009107412 hasConceptScore W3009107412C86803240 @default.
• W3009107412 hasConceptScore W3009107412C93237805 @default.
• W3009107412 hasConceptScore W3009107412C96765332 @default.
• W3009107412 hasFunder F4320320883 @default.
• W3009107412 hasIssue "15" @default.
• W3009107412 hasLocation W30091074121 @default.
• W3009107412 hasLocation W30091074122 @default.
• W3009107412 hasLocation W30091074123 @default.
• W3009107412 hasLocation W30091074124 @default.
• W3009107412 hasOpenAccess W3009107412 @default.
• W3009107412 hasPrimaryLocation W30091074121 @default.

• next