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

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

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...

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Bibliographic Details
Main Authors: Nicolas Lebouvier, Fabrice Pagniez, Young Min Na, Da Shi, Patricia Pinson, Mathieu Marchivie, Jean Guillon, Tarek Hakki, Rita Bernhardt, Sook Wah Yee, Claire Simons, Marie-Pierre Lézé, Rolf W. Hartmann, Angélique Mularoni, Guillaume Le Baut, Isabelle Krimm, Ruben Abagyan, Patrice Le Pape, Marc Le Borgne
Format: Article
Language:English
Published: MDPI AG 2020-08-01
Series:Pharmaceuticals
Subjects:
azoles
antifungal agents
indole
microwave irradiation
X-ray crystallography
<i>Candida</i> species
Online Access:https://www.mdpi.com/1424-8247/13/8/186

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https://www.mdpi.com/1424-8247/13/8/186

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