2015
DOI: 10.1016/j.bmc.2015.02.061
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Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice

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Cited by 20 publications
(23 citation statements)
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“…FClAQ1 even afforded complete cure. Such discordance has been previously reported for some thiophene-and furan-based aminoquinolines synthesized by the same group [24]. The discrepancy between in vitro and in vivo effects suggests that the antimalarial efficacy of such compounds is due to their metabolites, rather than the compounds themselves.…”
Section: Discussionmentioning
confidence: 64%
“…FClAQ1 even afforded complete cure. Such discordance has been previously reported for some thiophene-and furan-based aminoquinolines synthesized by the same group [24]. The discrepancy between in vitro and in vivo effects suggests that the antimalarial efficacy of such compounds is due to their metabolites, rather than the compounds themselves.…”
Section: Discussionmentioning
confidence: 64%
“…As the isomeric products 7 and 8 could be easily separated, we proceeded with further transformations. Vinyl bromides 7 and 8 and the previously synthesized thiepine 4 were successfully coupled with a series of arylboronic acids under Suzuki cross‐coupling reaction conditions, affording compounds 9 – 18 in moderate‐to‐excellent yields (Scheme ). The compound 7 was coupled with thiophenols via the palladium‐catalyzed reaction, using the 1,1′‐bis(diphenylphosphino)ferrocene (dppf) as a ligand, as shown in the Scheme .…”
Section: Resultsmentioning
confidence: 99%
“…Now, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting Plasmodium falciparum parasite growth and compare the obtained results with CQ and previously reported related thiophene and benzothiophene-based 4-amino-7-chloroquinoline derivatives [ 27 , 28 ], as well as other antimalarial benzothiophene derivatives.…”
Section: Introductionmentioning
confidence: 84%