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Updated: Jun 18, 2026

A High-throughput Compatible Assay to Evaluate Drug Efficacy against Macrophage Passaged Mycobacterium tuberculosis
Published on: March 24, 2017
Discovery of dipiperidines as new antitubercular agents
Elena Bogatcheva1, Colleen Hanrahan, Ping Chen
1Sequella, Inc., 9610 Medical center Drive, Suite 200, Rockville, MD 20850, USA. elenabogatcheva@sequella.com
None:
As part of our ongoing research effort to develop new therapeutics for treatment of tuberculosis (TB), we synthesized a combinatorial library of 10,358 compounds on solid support using a pool-and-split technique and tested the resulting compounds for activity against Mycobacteriumtuberculosis. Structure-activity relationship (SAR) evaluation identified new compounds with antitubercular activity, including a novel hit series that is structurally unrelated to any existing antitubercular drugs, dipiperidines. Dipiperidine representatives exhibited MIC values as low as 7.8microM, the ability to induce promoter Rv0341 activated in response to cell wall biosynthesis inhibition, relatively low nonspecific cellular toxicity in the range of 30-162microM, and logP values less than 4.
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