Related Experiment Video
Updated: Apr 15, 2026

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
Thiophene containing trisubstituted methanes [TRSMs] as identified lead against Mycobacterium tuberculosis
Priyanka Singh1, Sudipta Kumar Manna1, Amit Kumar Jana1
1Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, B.S. 10/1, Jankipuram Extension, Sitapur Road, Lucknow-226031, UP, India.
Abstract:
Triarylmethanes (TRAMs) and thiophene containing trisubstituted methanes (TRSMs) have been reported by us, having potential against Mycobacterium tuberculosis and Mycobacterium fortuitum strains, respectively. Further, extension through synthesis and biological evaluation of novel TRSMs resulted into an identified lead 36 (S006-830) [(diisopropyl-(2-{4-[(4-methoxy-phenyl)- thiophen-2-yl-methyl]-phenoxy}-ethyl)-amine)] with MIC: 1.33 mg/L, non-toxic against Vero C-1008 cell line with selectivity index >10, ex vivo efficacy equivalent to first line TB drugs-isoniazid (INH), rifampicin (RFM) and pyrazinamide (PZA) in the mouse and human macrophages, and lung CFU count of 2.2 × 10(7) (approximately 15 fold lesser than untreated mice, 31 × 10(7)) with efficacies comparable to ethambutol (EMB) (1.27 × 10(7)) and PZA (1.9 × 10(7)). Further, S006-830 also showed potent bactericidal activity against multi-drug resistant and single-drug resistant clinical isolates of M. tuberculosis.
More Related Videos
07:50Author Spotlight: Scalable Drug Screening Protocol for Efficient Discovery of M. abscessus Treatments
Published on: October 25, 2024
09:57Visualization of the Charcoal Agar Resazurin Assay for Semi-quantitative, Medium-throughput Enumeration of Mycobacteria
Published on: December 14, 2016
Related Concept Videos
Radical Substitution: Hydrogenolysis of Alkyl Halides with Tributyltin Hydride
The bonds formed in this reaction are stronger than the bonds broken, making it energetically favorable. The reaction follows a radical chain mechanism similar to radical halogenation...
Directing and Steric Effects in Disubstituted Benzene Derivatives
Electrophilic Aromatic Substitution: Fluorination and Iodination of Benzene
Pulmonary Tuberculosis V
Latent tuberculosis infection occurs when TB bacteria are present in a person's body, but are not causing illness or symptoms. It is not contagious, and preventive treatment is crucial to avoid the...