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In order to find novel antifungal agents with good activity and aqueous solubility,a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility.The results indicated that some compounds showed potent activity against six pathogenic fungi.In particular,the analogue 17a having an isobutyl substitution on the triazolone exhibited significant broad spectrum antifungal activity.In addition,the water solubility of compound 17a was sufficiently improved over SYN-2869.
In order to find novel antifungal agents with good activity and aqueous solubility, a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility. These results indicate that some compounds showed potent activity against six pathogenic fungi.In particular, the analogue 17a has an isobutyl substitution on the triazolone demonstrated significant broad spectrum antifungal activity. In addition, the water solubility of the compound 17a was significantly improved over SYN-2869.