title: In Vivo and In Vitro Optimization of Screening Antimalarial Hits toward Lead Molecules for Preclinical Development.
abstract: In order to overcome one of the greatest challenges in malaria treatment, drug resistance, new drug candidates are urgently needed, which should preferably act via novel mechanisms. Successful optimization of a phenotypic screening hit based on a quinoline-4-carboxamide derivative resulted in the highly promising lead structure 4, which according to the Medicines for Malaria Venture (MMV) met the efficacy and drug metabolism and pharmacokinetics (DMPK) requirements for a malaria drug target candidate and consequently was selected for preclinical development.
authors: Organic Chemistry Chair I and Interdisciplinary Center for Molecular Materials (ICMM), Friedrich-Alexander University of Erlangen-Nürnberg , Henkestrasse 42, 91054 Erlangen, Germany.
authors: Tony
authors: T
authors: Fröhlich
authors: Organic Chemistry Chair I and Interdisciplinary Center for Molecular Materials (ICMM), Friedrich-Alexander University of Erlangen-Nürnberg , Henkestrasse 42, 91054 Erlangen, Germany.
authors: Svetlana B
authors: SB
authors: Tsogoeva
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical / Q000379:methods* / Q000592:standards*; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D011804:Quinolines; C000619996:quinoline-4-carboxamide