Abstract
Twelve pyrrole hydrazones were synthesized and evaluated in vitro as inhibitors of Mycobacterium tuberculosis H37Rv with IC50 and IC90 to 5.92 μg/ml and 9.37 μg/ml respectively. The most active 12d (ethyl 5-(4-chlorophenyl)- 2-methyl-1-(4-(2-((5-nitrofuran-2-yl)methylene)hydrazinyl)-4-oxobutyl)-1H-pyrrole-3-carboxylate) has IC90 value of 9.372 μg/ml. The derived second order QSAR model favors moderate molecular surfaces in a combination with electronaccepting substituents in the aromatic hydrazone moiety.
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
Letters in Drug Design & Discovery
Title: Pyrrole-Based Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics
Volume: 7 Issue: 6
Author(s): Atanas Bijev and Maya Georgieva
Affiliation:
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
Abstract: Twelve pyrrole hydrazones were synthesized and evaluated in vitro as inhibitors of Mycobacterium tuberculosis H37Rv with IC50 and IC90 to 5.92 μg/ml and 9.37 μg/ml respectively. The most active 12d (ethyl 5-(4-chlorophenyl)- 2-methyl-1-(4-(2-((5-nitrofuran-2-yl)methylene)hydrazinyl)-4-oxobutyl)-1H-pyrrole-3-carboxylate) has IC90 value of 9.372 μg/ml. The derived second order QSAR model favors moderate molecular surfaces in a combination with electronaccepting substituents in the aromatic hydrazone moiety.
Export Options
About this article
Cite this article as:
Bijev Atanas and Georgieva Maya, Pyrrole-Based Hydrazones Synthesized and Evaluated In Vitro as Potential Tuberculostatics, Letters in Drug Design & Discovery 2010; 7 (6) . https://dx.doi.org/10.2174/157018010791306588
DOI https://dx.doi.org/10.2174/157018010791306588 |
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
-
Patented Biomarkers of Peripheral Blood for the Early Detection of Cancer
Recent Patents on Biomarkers CYP1A2, CYP2A6, CYP2B6, CYP3A4 and CYP3A5 Polymorphisms in Two Bantu-Speaking Populations from Cameroon and South Africa: Implications for Global Pharmacogenetics
Current Pharmacogenomics and Personalized Medicine Cystic Hygroma with Multiple Benign Bone Lymphangiomas in an Adult Patient: A Rare Entity in the Differential Diagnosis of Multiple Osseous Lesions in Oncology Practice
Current Medical Imaging The Balancing Act between Colonisers and Inflammation: T regulatory and TH17 Cells in Mucosal Immunity during Otitis Media
Current Immunology Reviews (Discontinued) Computer-Aided Discovery in Antimicrobial Research: In Silico Model for Virtual Screening of Potent and Safe Anti-Pseudomonas Agents
Combinatorial Chemistry & High Throughput Screening Heterocyclic Chalcone Analogues as Potential Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Editorial [Hot topic: Structure-Based Virtual Screening (Guest Editor: Walter Filgueira De Azevedo Jr.)]
Current Drug Targets Allelic Imbalances of the egfr Gene as Key Events in Breast Cancer Progression – the Concept of Committed Progenitor Cells
Current Cancer Drug Targets Nanotechnology for Delivery of Drugs and Biomedical Applications
Current Clinical Pharmacology Interethnic and Intraethnic Variability of NAT2 Single Nucleotide Polymorphisms
Current Drug Metabolism Anti-Microbial
Current Bioactive Compounds An Evidence-Based Review of the Mechanism of Action, Efficacy, and Safety of Biologic Therapies in the Treatment of Psoriasis and Psoriatic Arthritis
Current Medicinal Chemistry TNF-α and Ghrelin: Opposite Effects on Immune System, Metabolism and Mental Health
Protein & Peptide Letters Proteases and Their Role in Chronic Inflammatory Lung Diseases
Current Drug Targets Editorial from Guest Editor [Hot Topic:Vitamin D and Respiratory Health (Guest Editor: Adrian R. Martineau)]
Current Respiratory Medicine Reviews Exploration of Ion Channels in Mycobacterium tuberculosis: Implication on Drug Discovery and Potent Drug Targets Against Tuberculosis
Current Chemical Biology COVID-19: Are Experimental Drugs a Cure or Cause?
Current Drug Safety Synthesis and Antibacterial Activity of Mefloquine-Based Analogs Against Sensitive and Resistant Mycobacterium tuberculosis Strains
Current Topics in Medicinal Chemistry The Role of Oxazolidine Derivatives in the Treatment of Infectious and Chronic Diseases
Current Bioactive Compounds An Overview of the Carbonic Anhydrases from Two Pathogens of the Oral Cavity: Streptococcus mutans and Porphyromonas gingivalis
Current Topics in Medicinal Chemistry