Iodine-Mediated Cascade Amination Enables One-pot Access to Antimicrobial Indole-Embedded Dihydropyrazoles
Abstract
A metal-free, iodine-mediated amination enables a one-pot synthesis of indole-embedded dihydropyrazoles with broad substrate scope. The lead compound 5qq exhibited potent antimicrobial activity (MIC = 4 µg/mL) via DNA gyrase inhibition, showed efficient bacterial uptake, and displayed negligible cytotoxicity up to 100 µM, highlighting its promise as an antimicrobial lead.
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