Synthesis, Optimization, Antifungal Activity, Selectivity, and CYP51 Binding of New 2-Aryl-3-azolyl-1-indolyl-propan-2-ols

• Main Authors: Nicolas Lebouvier (Author), Fabrice Pagniez (Author), Young Min Na (Author), Da Shi (Author), Patricia Pinson (Author), Mathieu Marchivie (Author), Jean Guillon (Author), Tarek Hakki (Author), Rita Bernhardt (Author), Sook Wah Yee (Author), Claire Simons (Author), Marie-Pierre Lézé (Author), Rolf W. Hartmann (Author), Angélique Mularoni (Author), Guillaume Le Baut (Author), Isabelle Krimm (Author), Ruben Abagyan (Author), Patrice Le Pape (Author), Marc Le Borgne (Author)
• Format: Book
• Published: MDPI AG, 2020-08-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

A series of 2-aryl-3-azolyl-1-indolyl-propan-2-ols was designed as new analogs of fluconazole (FLC) by replacing one of its two triazole moieties by an indole scaffold. Two different chemical approaches were then developed. The first one, in seven steps, involved the synthesis of the key intermediat...