{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Basilico N"],"funding":["MIUR-PRIN,Italy","EU-FP6 AntiMal","COST Action"],"pagination":["E2102"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6149971"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["22(12)"],"pubmed_abstract":["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. f"],"journal":["Molecules (Basel, Switzerland)"],"pubmed_title":["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."],"pmcid":["PMC6149971"],"funding_grant_id":["2010C2LKKJ_006","20154JRJPP_004","IP-018834","CM1307"],"pubmed_authors":["Russell B","Dondio G","Lucantoni L","Renia L","Nosten F","Vivas L","Suwanarusk R","Habluetzel A","Misiano P","Romeo S","Yardley V","Bigogno C","Taramelli D","Basilico N","Sparatore A","Parapini S","Croft SL","Jabes D"],"additional_accession":[]},"is_claimable":false,"name":"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.","description":"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. f","dates":{"release":"2017-01-01T00:00:00Z","publication":"2017 Dec","modification":"2026-05-02T05:09:49.743Z","creation":"2019-03-27T00:07:07Z"},"accession":"S-EPMC6149971","cross_references":{"pubmed":["29194347"],"doi":["10.3390/molecules22122102"]}}