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 a broad substrate scope. The lead compound 5qq exhibited potent antimicrobial activity (MIC = 4 µg mL⁻¹) via DNA gyrase inhibition, showed efficient bacterial uptake, and displayed negligible cytotoxicity up to 100 µM, highlighting its promise as an antimicrobial lead.