ArticleAntimicrobial agents and chemotherapy2021
Biological and Biochemical Evaluation of Isatin-Isoniazid Hybrids as Bactericidal Candidates against
Article in Antimicrobial agents and chemotherapy, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Who cites it
7 citing papers in PubMed, 22 citations in OpenAlex.
- Bioinformatics and experimental analysis identify CHN2 and MEF2C as diagnostic biomarkers for tuberculosis.American journal of translational research · 2026Article
- Isoniazid-rhodanine molecular hybrids: design, synthesis, antimycobacterial activity and computational validation.RSC advances · 2025Article
- Rational design and microwave-promoted synthesis of triclosan-based dimers: targeting InhA for anti-mycobacterial profiling.Royal Society open science · 2024Article
- Cu-promoted synthesis of triclosan-Mannich and Glaser adducts: anti-mycobacterial evaluation withFuture medicinal chemistry · 2024Article
- Tailoring selective triclosan azo-adducts: Design, synthesis, and anti-mycobacterial evaluation.Heliyon · 2023Article
- A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs).Pharmaceuticals (Basel, Switzerland) · 2022Review
- Synthetic approaches to potent heterocyclic inhibitors of tuberculosis: A decade review.Frontiers in pharmacology · 2022Review
Corrections and comments
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Authors and funding
9 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tuberculosis remains a leading cause of mortality among infectious diseases worldwide, prompting the need to discover new drugs to fight this disease. We report here the design, synthesis, and antimycobacterial activity of isatin-mono/bis-isoniazid hybrids. Most of the compounds exhibited very high activity against Mycobacterium tuberculosis, with MICs in the range of 0.195 to 0.39 μg/ml, and exerted a more potent bactericidal effect than the standard antitubercular drug isoniazid (INH). Importantly, these compounds were found to be well tolerated at high doses (>200 μg/ml) on Vero kidney cells, leading to high selectivity indices. Two of the most promising hybrids were evaluated for activity in THP-1 macrophages infected with M. tuberculosis, among which compound 11e was found to be slightly more effective than INH. Overexpression of InhA along with cross-resistance determination of the most potent compounds, selection of resistant mutants, and biochemical analysis, allowed us to decipher their mode of action. These compounds effectively inhibited mycolic acid biosynthesis and required KatG to exert their biological effects. Collectively, this suggests that the synthesized isatin-INH hybrids are promising antitubercular molecules for further evaluation in preclinical settings.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.