biostudies-literatureBasilico NMIUR-PRIN,ItalyEU-FP6 AntiMalCOST ActionE2102https://www.ebi.ac.uk/biostudies/studies/S-EPMC6149971biostudies-literatureUnknown22(12)Natural products are a prolific source for the identification of new biologically active compounds. In the present work, we studied the in vitro and in vivo antimalarial efficacy and ADME-Tox profile of a molecular hybrid (AM1) between 4-aminoquinoline and a quinolizidine moiety derived from lupinine (<i>Lupinus luteus</i>). The aim was to find a compound endowed with the target product profile-1 (TCP-1: molecules that clear asexual blood-stage parasitaemia), proposed by the Medicine for Malaria Venture to accomplish the goal of malaria elimination/eradication. AM1 displayed a very attractive profile in terms of both in vitro and in vivo activity. By using standard in vitro antimalarial assays, AM1 showed low nanomolar inhibitory activity against chloroquine-sensitive and resistant <i>P. fMolecules (Basel, Switzerland)In Vivo and In Vitro Activities and ADME-Tox Profile of a Quinolizidine-Modified 4-Aminoquinoline: A Potent Anti-P. falciparum and Anti-P. vivax Blood-Stage Antimalarial.PMC61499712010C2LKKJ_00620154JRJPP_004IP-018834CM1307Russell BDondio GLucantoni LRenia LNosten FVivas LSuwanarusk RHabluetzel AMisiano PRomeo SYardley VBigogno CTaramelli DBasilico NSparatore AParapini SCroft SLJabes DfalseIn Vivo and In Vitro Activities and ADME-Tox Profile of a Quinolizidine-Modified 4-Aminoquinoline: A Potent Anti-P. falciparum and Anti-P. vivax Blood-Stage Antimalarial.Natural products are a prolific source for the identification of new biologically active compounds. In the present work, we studied the in vitro and in vivo antimalarial efficacy and ADME-Tox profile of a molecular hybrid (AM1) between 4-aminoquinoline and a quinolizidine moiety derived from lupinine (<i>Lupinus luteus</i>). The aim was to find a compound endowed with the target product profile-1 (TCP-1: molecules that clear asexual blood-stage parasitaemia), proposed by the Medicine for Malaria Venture to accomplish the goal of malaria elimination/eradication. AM1 displayed a very attractive profile in terms of both in vitro and in vivo activity. By using standard in vitro antimalarial assays, AM1 showed low nanomolar inhibitory activity against chloroquine-sensitive and resistant <i>P. f2017-01-01T00:00:00Z2017 Dec2026-05-02T05:09:49.743Z2019-03-27T00:07:07ZS-EPMC61499712919434710.3390/molecules22122102