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.