Details

Autor(en) / Beteiligte

• Jad, Yahya E.
• Acosta, Gerardo A.
• Naicker, Tricia
• Ramtahal, Melissa
• El-Faham, Ayman
• Govender, Thavendran
• Kruger, Hendrik G.
• Torre, Beatriz G. de la
• Albericio, Fernando

Titel

Synthesis and Biological Evaluation of a Teixobactin Analogue

Ist Teil von

• Organic letters, 2015-12, Vol.17 (24), p.6182-6185

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2015

Quelle

MEDLINE

Beschreibungen/Notizen

• The first synthesis and biological activity of a teixobactin analogue is reported. Substitution of the unusual l-allo-enduracididine residue by the naturally occurring l-arginine was achieved, and the analogue gave an activity trend similar to that of teixobactin (against Gram-postive bacteria) and meropenem, which was approved by the FDA in 1996. The synthetic route used allows for the synthesis of the natural product as well as the development of a program of medicinal chemistry.