Design and synthesis of spiro[pyrrolidine-3,3'-quinoline]-2,2'-dione derivatives as novel antifungal agents targeting chitin synthase.

A novel spiro [pyrrolidine-3',3'-quinoline]-2,2'-dione scaffold was constructed using fragments of quinoline and pyrrolidine. Subsequently, two series of derivatives were designed based on this scaffold. The enzyme inhibition experiments revealed that all designed compounds had moderate to good inhibitory activity against chitin synthase (CHS).

Spiro[benzoxazine-piperidin]-one derivatives as chitin synthase inhibitors and antifungal agents: Design, synthesis and biological evaluation.

Four series of spiro[benzoxazine-piperidin]-one derivatives were designed and synthesized. Their inhibition percentages against chitin synthase and antifungal activities were evaluated. Based on the preliminary biological assays, the series of derivatives containing α, β-unsaturated carbonyl fragment which had moderate to excellent CHS inhibitory activity and antifungal activity were further researched.