Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl) amino]-2-phenyl-3-(1H-1, 2, 4-triazol-1-yl) propan-2-ols

…, M Le Borgne, C Picot, F Pagniez, P Le Pape

Index: Guillon, Remi; Giraud, Francis; Loge, Cedric; Le Borgne, Marc; Picot, Carine; Pagniez, Fabrice; Le Pape, Patrice Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 20 p. 5833 - 5836

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Citation Number: 17

Abstract

We previously reported on the design and synthesis of 1-[((hetero) aryl-or piperidinylmethyl) amino]-2-phenyl-3-(1H-1, 2, 4-triazol-1-yl) propan-2-ols showing various degrees of antifungal activity against Candida albicans and Aspergillus fumigatus strains. Now we have identified a series of 1-[(1H-indol-5-ylmethyl) amino] derivatives which exhibited potent MICs (< 65ngmL− 1) against C. albicans strain. The synthesis and SAR behind the indole ...