Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II
- Author
- MUTHAS, Daniel1 ; NÖBTEBERG, Daniel1 ; SABNIS, Yogesh A1 ; HAMELINK, Elizabeth2 ; VRANG, Lotta2 ; SAMUELSSON, Bertil2 ; KARLEN, Anders1 ; HALLBERG, Anders1
[1] Department of Medicinal Chemistry, Uppsala University. Box 574, 751 23 Uppsala, Sweden
[2] Medivir AB, Lunastigen 7, 14144 Huddinge, Sweden - Source
Bioorganic & medicinal chemistry. 2005, Vol 13, Num 18, pp 5371-5390, 20 p ; ref : 40 ref
- ISSN
- 0968-0896
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier Science, Oxford
- Publication country
- United Kingdom
- Document type
- Article
- Language
- English
- Author keyword
- Hydroxyethylamine Malaria Molecular modeling Plasmepsin
- Keyword (fr)
- Aminoalcool Aminoamide Antipaludique Antiparasitaire Antiprotozoaire Carboxamide Complexe enzyme inhibiteur Composé non peptide Composé peptidomimétique Etat transition Inhibiteur enzyme Modèle 3 dimensions Modèle moléculaire Modélisation Médicament ciblé Méthode CoMFA Plasmepsin Plasmodium falciparum Prédiction Pyridine dérivé Relation structure activité Site actif Synthèse chimique Apicomplexa Aspartic endopeptidases Enzyme Hydrolases Peptidases Protozoa
- Keyword (en)
- Aminoalcohol Aminoamide Antimalarial Parasiticide Antiprotozoal agent Carboxamide Inhibitor enzyme complex Non peptide compound Peptidomimetic compound Transition state Enzyme inhibitor Three dimensional model Molecular model Modeling Targeted drug Comparative molecular field analysis method Plasmepsin Plasmodium falciparum Prediction Pyridine derivatives Structure activity relation Active site Chemical synthesis Apicomplexa Aspartic endopeptidases Enzyme Hydrolases Peptidases Protozoa
- Keyword (es)
- Aminoalcohol Aminoamida Antipalúdico Antiparasitario Antiprotozoario Carboxamida Complejo enzima inhibidor Compuesto no péptido Compuesto peptidomimético Estado transitorio Inhibidor enzima Modelo 3 dimensiones Modelo molecular Modelización Medicamento dirigido Método CoMFA Plasmepsin Plasmodium falciparum Predicción Piridina derivado Relación estructura actividad Lugar activo Síntesis química Apicomplexa Aspartic endopeptidases Enzima Hydrolases Peptidases Protozoa
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02S Antibiotics. Antiinfectious agents. Antiparasitic agents / 002B02S06 Antiparasitic agents
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 17015907
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1016/j.bmc.2005.06.048 
https://dx.doi.org/10.1016/j.bmc.2005.06.048
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