Abstract
AbstractIn last three decades, only one new USFDA approved antifungal drug (echinocandin) was introduced into the clinics. The identification of new scaffolds with novel mechanisms of action is an important goal of current antifungal research. Herein, we describe the design, synthesis and in vitro antimicrobial activities of heterocycle‐His(2‐aryl)‐Arg‐NHBzl conjugates as a new structural class of peptidomimetics with promising antifungal activity against Cryptococcus neoformans (IC50 values ranging between 2.13–14.57 μg mL−1). The most potent analog, quinolinyl‐His(2‐tert‐butylphenyl)‐Arg‐NHBzl (17 f) exhibited IC50 and MIC values of 2.13 and 2.50 μg mL−1, respectively against C. neoformans.
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