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Updated: May 18, 2026

Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
Allylic thiocyanates as a new class of antitubercular agents
Gustavo P Silveira1, Misael Ferreira, Luciano Fernandes
1Departamento de Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Abstract:
TB is a global public health emergency in which new drugs are desperately needed. Herein we report on the synthesis of a diverse panel of 41 aryl allylic azides, thiocyanates, isothiouronium salts, and N,N'-diacetylisothioureas that were evaluated for their in vitro activity against replicating and non-replicating Mycobacterium tuberculosis (Mtb) H(37)Rv and toxicity to VERO cells. We found a selective group of new and promising compounds having good (micromolar) to excellent (sub-micromolar) potency against replicating Mtb H(37)Rv. Allylic thiocyanates bearing halophenyl (halo=2-Br, 4-Br, 4-Cl, 4-F), 4-methylphenyl and 2-naphthyl moieties were the most active as antitubercular agents. In particular, the 2-bromophenyl-substituted thiocyanate showed MIC=0.25 μM against replicating Mtb, MIC=8.0 μM against non-replicating Mtb and IC(50)=32 μM in the VERO cellular toxicity assay.
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