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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Article information

Article type
Communication
Submitted
12 Jan 2026
Accepted
11 Mar 2026
First published
14 Mar 2026

Org. Biomol. Chem., 2025, Accepted Manuscript

Iodine-Mediated Cascade Amination Enables One-pot Access to Antimicrobial Indole-Embedded Dihydropyrazoles

A. Krishna, K. T. Ashitha, M. P. Bhat, M. Rudrappa, A. C. Santhoshkumar, L. Basha, S. Varughese, N. Vankadari, S. Nayaka and B. S. Sasidhar, Org. Biomol. Chem., 2025, Accepted Manuscript , DOI: 10.1039/D6OB00043F

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