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Back Cover: Discovery and Characterization of ACT‐451840: an Antimalarial Drug with a Novel Mechanism of Action (ChemMedChem 18/2016)
Author(s) -
Boss Christoph,
Aissaoui Hamed,
Amaral Nathalie,
Bauer Aude,
Bazire Stephanie,
Binkert Christoph,
Brun Reto,
Bürki Cédric,
Ciana ClaireLise,
Corminboeuf Olivier,
Delahaye Stephane,
Dollinger Claire,
Fischli Christoph,
Fischli Walter,
Flock Alexandre,
Frantz MarieCéline,
Girault Malory,
Grisostomi Corinna,
Friedli Astrid,
Heidmann Bibia,
Hinder Claire,
Jacob Gael,
Le Bihan Amelie,
Malrieu Sophie,
Mamzed Saskia,
Merot Aurelien,
Meyer Solange,
Peixoto Sabrina,
Petit Nolwenn,
Siegrist Romain,
Trollux Julien,
Weller Thomas,
Wittlin Sergio
Publication year - 2016
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201600436
Subject(s) - artemisinin , drug discovery , phenotypic screening , pharmacology , computational biology , drug , mode of action , mechanism of action , drug action , chemistry , plasmodium falciparum , biology , malaria , biochemistry , in vitro , immunology , gene , phenotype
The back cover picture shows the successful collaboration between the Swiss TPH and Actelion Pharmaceuticals Ltd from the phenotypic screening hit via animal experiments to the antimalarial clinical candidate ACT‐451840, exhibiting a novel, yet unknown, mode of action. The quest for novel antimalarials has become urgent due to the first observed resistance developments against Artemisinin Combination Therapies (ACT). Extensive structure–activity investigation work ( P. falciparum NF54 and K1 and P. berghei ) and thorough in vivo pharmacokinetic and pharmacological characterization of several compounds were performed. In addition, discovery safety assessments and side‐effect potentials of key derivatives were evaluated. More information can be found in the Full Paper by Christoph Boss et al. on page 1995 in Issue 18, 2016 (DOI: 10.1002/cmdc.2016600298).