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Synthesis and biological properties of macrolactam analogs of the natural product macrolide (−)-A26771B
Authors:Sophie CanovaRenaud Lé  pine,Amber ThysAnne Baron,Didier Roche
Affiliation:a Galapagos, 102 Avenue Gaston Roussel, 93230 Romainville, France
b Edelris, 115 Avenue Lacassagne, 69003 Lyon, France
c Galapagos, Industriepark Mechelen Noord, General De Wittelaan L11 A3, B-2800 Mechelen, Belgium
Abstract:Promising synthetic derivatives of macrolactone natural product (−)-A26771B have been designed and synthesized both from semisynthesis and total synthesis. Further optimization led to the first synthesis of macrolactam analogs of (−)-A26771B with improved antibacterial activity and metabolic stability.
Keywords:Natural products   (&minus  )-  boldFont"  >A26771B   Antibacterial   Macrolactams   Metathesis
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