Abstract
During our investigation in the area of antimycobacterial agents, we have identified the 1,5-(4-chlorophenyl)-2- methyl-3-(4-methylpiperazin-1-yl)methyl-1H-pyrrole (BM212) as the lead compound for a new class of antimycobacterial pyrrole derivatives with potent in vitro activity against mycobacteria and with low cytotoxicity. We have also identified the salient structural features of BM212, while structure-activity relationships (SAR) and molecular modeling studies on pyrrole compounds allowed us to design and synthesize additional analogues. Among them, seven compounds revealed a very high activity (better than that of BM212 toward mycobacteria) and a very interesting protection index, comparable to that of reference compounds, such as isoniazid, streptomycin and rifampin.
Keywords: BM212, lead compound, mycobacterium tuberculosis, atypical mycobacteria, in vitro activity, intramacrophagic activity, pyrroles, pharmacophore, cytotoxicity, protection index
Mini-Reviews in Medicinal Chemistry
Title: New Derivatives of BM212: A Class of Antimycobacterial Compounds Based on the Pyrrole Ring as a Scaffold
Volume: 7 Issue: 1
Author(s): M. Biava, G. C. Porretta and F. Manetti
Affiliation:
Keywords: BM212, lead compound, mycobacterium tuberculosis, atypical mycobacteria, in vitro activity, intramacrophagic activity, pyrroles, pharmacophore, cytotoxicity, protection index
Abstract: During our investigation in the area of antimycobacterial agents, we have identified the 1,5-(4-chlorophenyl)-2- methyl-3-(4-methylpiperazin-1-yl)methyl-1H-pyrrole (BM212) as the lead compound for a new class of antimycobacterial pyrrole derivatives with potent in vitro activity against mycobacteria and with low cytotoxicity. We have also identified the salient structural features of BM212, while structure-activity relationships (SAR) and molecular modeling studies on pyrrole compounds allowed us to design and synthesize additional analogues. Among them, seven compounds revealed a very high activity (better than that of BM212 toward mycobacteria) and a very interesting protection index, comparable to that of reference compounds, such as isoniazid, streptomycin and rifampin.
Export Options
About this article
Cite this article as:
Biava M., Porretta C. G. and Manetti F., New Derivatives of BM212: A Class of Antimycobacterial Compounds Based on the Pyrrole Ring as a Scaffold, Mini-Reviews in Medicinal Chemistry 2007; 7 (1) . https://dx.doi.org/10.2174/138955707779317786
DOI https://dx.doi.org/10.2174/138955707779317786 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
- 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
-
Lipoxygenase (LOX) Pathway: A Promising Target to Combat Cancer
Current Pharmaceutical Design The 18 kDa Translocator Protein (TSPO): A New Perspective in Mitochondrial Biology
Current Molecular Medicine MicroRNAs in Lymphoma: Regulatory Role and Biomarker Potential
Current Genomics Bee Venom: Its Potential Use in Alternative Medicine
Anti-Infective Agents Can γH2AX be Used to Personalise Cancer Treatment?
Current Molecular Medicine Performance of Feature Selection Methods
Current Genomics Delineation of Current Development of Antimitotic Compounds Targeting Cytoskeletal Protein Tubulin and Microtubule in the Cancer Therapy
Current Chemical Biology Viral Induced Oxidative and Inflammatory Response in Alzheimer’s Disease Pathogenesis with Identification of Potential Drug Candidates: A Systematic Review using Systems Biology Approach
Current Neuropharmacology Unfolded Protein Response in Chronic Obstructive Pulmonary Disease: Smoking, Aging and Disease: A SAD Trifecta
Current Molecular Medicine Multifaceted Mechanisms for Cell Survival and Drug Targeting in Chronic Myelogenous Leukemia
Current Cancer Drug Targets Metal Protein Attenuating Compounds (MPACs): An Emerging Approach for the Treatment of Neurodegenerative Disorders
Current Bioactive Compounds Current and Emerging Therapeutic Approaches in HCV-Related Mixed Cryoglobulinemia
Current Medicinal Chemistry Involvement of Cannabinoids in Cellular Proliferation
Mini-Reviews in Medicinal Chemistry Suicide Gene Therapy Mediated by the Herpes Simplex Virus Thymidine Kinase Gene / Ganciclovir System: Fifteen Years of Application
Current Gene Therapy Recombinant Antibodies in Cancer Therapy
Current Protein & Peptide Science Anticancer Activities and Mechanisms of Bisdioxopiperazine Compounds Probimane and MST-16
Anti-Cancer Agents in Medicinal Chemistry Glycerophospholipid Synthesis as a Novel Drug Target Against Cancer
Current Molecular Pharmacology Targeting the Mevalonate Pathway for Improved Anticancer Therapy
Current Cancer Drug Targets Targeting Histone Deacetylases in Neuroblastoma
Current Pharmaceutical Design Identification of Two Novel Mutations in the <i>ATM</i> Gene from Patients with Ataxia-Telangiectasia by Whole Exome Sequencing
Current Genomics