Abstract
Fifteen new hydrazones were synthesized as derivatives of 1H-1-pyrrolylcarbohydrazides. Six products exhibited 73-98% inhibition against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL using Microplate Alamar Blue Assay, the most active evaluated at HTS Level 2 with IC50=0.966 and IC90=3.236. The activities correlate with molecular volumes in simplified second order QSAR model.
Keywords: Carbohydrazides, Hydrazones, Pyrrole, QSAR, Synthesis, Tuberculostatics
Letters in Drug Design & Discovery
Title: Synthesis, In Vitro Evaluations and Structure-Activity Assessment of Pyrrole Hydrazones as Potential Tuberculostatics
Volume: 5 Issue: 1
Author(s): A. Bijev
Affiliation:
Keywords: Carbohydrazides, Hydrazones, Pyrrole, QSAR, Synthesis, Tuberculostatics
Abstract: Fifteen new hydrazones were synthesized as derivatives of 1H-1-pyrrolylcarbohydrazides. Six products exhibited 73-98% inhibition against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL using Microplate Alamar Blue Assay, the most active evaluated at HTS Level 2 with IC50=0.966 and IC90=3.236. The activities correlate with molecular volumes in simplified second order QSAR model.
Export Options
About this article
Cite this article as:
Bijev A., Synthesis, In Vitro Evaluations and Structure-Activity Assessment of Pyrrole Hydrazones as Potential Tuberculostatics, Letters in Drug Design & Discovery 2008; 5 (1) . https://dx.doi.org/10.2174/157018008783406651
DOI https://dx.doi.org/10.2174/157018008783406651 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Medicinal Plants for the Prevention and Treatment of Bacterial Infections
Current Pharmaceutical Design Personalized and Predictive Medicine in Turkey: A Symposium Report of the Istanbul Working Group on Personalized Medicine, Istanbul, Turkey, September 10-12, 2009
Current Pharmacogenomics and Personalized Medicine Chagas Disease: Progress and New Perspectives
Current Medicinal Chemistry Advancements in Devices and Particle Engineering in Dry Powder Inhalation Technology
Current Topics in Medicinal Chemistry State of the Art Review and Report of New Tool for Drug Discovery
Current Topics in Medicinal Chemistry The Digenea Parasite Opisthorchis felineus: A Target for the Discovery and Development of Novel Drugs
Infectious Disorders - Drug Targets Unleashing the Potential of Microbial Natural Products in Drug Discovery: Focusing on <i>Streptomyces</i> as Antimicrobials Goldmine
Current Topics in Medicinal Chemistry Adverse Effects and Drug Interactions of Biologic Agents
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Systemic Vasculitis: An Epidemiological Perspective
Current Immunology Reviews (Discontinued) Progress in Nanoparticulate Systems for Peptide, Proteins and Nucleic Acid Drug Delivery
Current Pharmaceutical Biotechnology Periodic Correlation Structures in Bacterial and Archaeal Complete Genomes
Current Bioinformatics RNA Sensors as a Mechanism of Innate Immune Evasion among SARSCoV2, HIV and Nipah Viruses
Current Protein & Peptide Science Patent Selections
Recent Patents on Anti-Infective Drug Discovery Early Life Vitamin D Status and Lung Development
Current Respiratory Medicine Reviews Nasal Vaccines Against Hepatitis B: An Update
Current Pharmaceutical Biotechnology Biomedical Applications of Natural Polymers for Drug Delivery
Current Organic Chemistry Bacterial Cell Division Regulation by Ser/Thr Kinases: A Structural Perspective
Current Protein & Peptide Science HIV-Specific T Cells: Strategies for Fighting a Moving Target
Current HIV Research Oxazolidinone Antibacterials and Our Experience
Anti-Infective Agents in Medicinal Chemistry Biopolymer Catalysed Synthesis of 6-methyl-4-phenylcarbamoyl-1, 2, 3, 4- Tetrahydropyrimidine-2-ones and Evaluation of their Anti-bacterial and Anti-tubercular Activities
Current Bioactive Compounds