Design, synthesis and structure-activity relationship study of wollamide B; a new potential anti TB agent

Wollamide B is a cationic antimycobacterial cyclohexapeptide that exhibits activity against Mycobacterium bovis (M. bovis) (IC50 of 3.1 μM). Aiming to define its structural activity relationship (SAR), optimizing potency and pharmacokinetic properties, libraries of analogues were synthesized followi...

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Veröffentlicht in:	PloS one 2017-04, Vol.12 (4), p.e0176088-e0176088
Hauptverfasser:	Asfaw, Henok, Laqua, Katja, Walkowska, Anna Maria, Cunningham, Fraser, Martinez-Martinez, Maria Santos, Cuevas-Zurita, Juan Carlos, Ballell-Pages, Lluís, Imming, Peter
Format:	Artikel
Sprache:	eng
Schlagworte:	Albumin Amino acid composition Amino acid sequence Amino acids AMP Animals Antimicrobial activity Antimicrobial agents Antimicrobial peptides Antitubercular Agents - blood Antitubercular Agents - chemical synthesis Antitubercular Agents - pharmacokinetics Antitubercular Agents - pharmacology Arginine Bacteria Bioavailability Biochemistry Biodegradation Biological activity Biological membranes Biology and Life Sciences Bone marrow Cell envelopes Cell survival Cell Survival - drug effects Chemistry Defensive behavior Degradation Drug Design Drug resistance Drugs Half-Life Hep G2 Cells Humans Immune system Immunogenicity Infectious diseases Interfaces Intestine Lipid bilayers Lipid membranes Lipids Liquid chromatography Magnetohydrodynamic stability Medicine and Health Sciences Membranes Metabolism Methylation Mice Microbial Sensitivity Tests Mode of action Molecular weight Multidrug resistance Mycobacterium tuberculosis - drug effects Mycobacterium tuberculosis - growth & development Nutrition Optimization Pathogens Peptides Peptides, Cyclic - blood Peptides, Cyclic - chemical synthesis Peptides, Cyclic - pharmacokinetics Peptides, Cyclic - pharmacology Permeability Pharmaceutical sciences Pharmacokinetics Phosphates Physical Sciences Protecting groups Research and Analysis Methods Solid phases Solubility Species Specificity Structure-Activity Relationship Synthesis Tuberculosis
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