Abstract
Design, results of in vitro antimycobacterial evaluation, and study of structure-activity relationships of various pyrazinecarboxylic acid reversible derivatives are presented. This review deals with some pyrazinamide analogues/prodrugs derived from Nphenylpyrazine- 2-carboxamides (1), arylaminopyrazine-2,5-dicarbonitriles (2), aryl/alkylsulphanylpyrazines (3,4), and aroylpyrazines (5) effecting > 50% inhibition in the primary antimycobacterial screen. The promising pyrazine candidates for further antimycobacterial evaluation were discovered. Results give good view onto structure-activity relationships of these analogues and promise even better activity of new compounds prepared after some structure optimization experiments.
Keywords: Pyrazines, in vitro antimycobacterial evaluation, structure-activity relationships, Tuberculosis, pyridine, esters, amide prodrugs, MIC (Minimal Inhibitory Concentration), Lawesson's reagent, Homolytic aroylation
Current Pharmaceutical Design
Title: Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives
Volume: 17 Issue: 32
Author(s): Martin Dolezal, Diana Kesetovic and Jan Zitko
Affiliation:
Keywords: Pyrazines, in vitro antimycobacterial evaluation, structure-activity relationships, Tuberculosis, pyridine, esters, amide prodrugs, MIC (Minimal Inhibitory Concentration), Lawesson's reagent, Homolytic aroylation
Abstract: Design, results of in vitro antimycobacterial evaluation, and study of structure-activity relationships of various pyrazinecarboxylic acid reversible derivatives are presented. This review deals with some pyrazinamide analogues/prodrugs derived from Nphenylpyrazine- 2-carboxamides (1), arylaminopyrazine-2,5-dicarbonitriles (2), aryl/alkylsulphanylpyrazines (3,4), and aroylpyrazines (5) effecting > 50% inhibition in the primary antimycobacterial screen. The promising pyrazine candidates for further antimycobacterial evaluation were discovered. Results give good view onto structure-activity relationships of these analogues and promise even better activity of new compounds prepared after some structure optimization experiments.
Export Options
About this article
Cite this article as:
Dolezal Martin, Kesetovic Diana and Zitko Jan, Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives, Current Pharmaceutical Design 2011; 17 (32) . https://dx.doi.org/10.2174/138161211798194477
DOI https://dx.doi.org/10.2174/138161211798194477 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
- 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
- Announcements
Related Articles
-
New Strategies in Drug Development Focusing on the Anti-Protease- Protease Balance in Alpha-1 Antitrypsin Deficiency
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Structural Analysis of Dihydrofolate Reductase and Thymidylate Synthase from Mammalian and Pathogenic Organisms
Current Enzyme Inhibition Application of Sulfamic Acid in Organic Synthesis-A Short Review
Current Organic Chemistry Graphical Abstracts
Letters in Drug Design & Discovery Novel Antibacterial Compounds and their Drug Targets - Successes and Challenges
Current Medicinal Chemistry Effective Therapy with the Neuroleptic Thioridazine as an Adjunct to Second Line of Defence Drugs, and the Potential that Thioridazine Offers for New Patents that Cover a Variety of “New Uses”
Recent Patents on Anti-Infective Drug Discovery Identification of Anti-cancer Peptides Based on Multi-classifier System
Combinatorial Chemistry & High Throughput Screening Prophylactic Admission of an In Vitro Reconstructed Complexes of Human Recombinant Heat Shock Proteins and Melanoma Antigenic Peptides Activates Anti-Melanoma Responses in Mice
Current Molecular Medicine Older Adults Prescribed Methadone: A Review of the Literature Across the Life Span from Opiate Initiation to Methadone Maintenance Treatment
Current Drug Abuse Reviews Structure and Function of Enzymes of Shikimate Pathway
Current Bioinformatics Fluoroquinolones: Blessings Or Curses
Current Drug Targets Meet Our Editorial Board Member
Combinatorial Chemistry & High Throughput Screening “Nano-Biomaterials” – A New Approach Concerning Multi-Drug Resistant Tuberculosis (MDR-TB)
Pharmaceutical Nanotechnology Antimicrobial Potentials, Phytochemical Screening and Determination of Bioactive Compounds from Three Indian Folk Medicinal Plants
Current Bioactive Compounds The Role of Hyphenated Chromatography-Mass Spectrometry Techniques in Exploratory Drug Metabolism and Pharmacokinetics
Current Pharmaceutical Design A Comprehensive Review on the Biological and Pharmacological Activities of Rhodanine Based Compounds for Research and Development of Drugs
Mini-Reviews in Medicinal Chemistry Synthesis and Biological Evaluation of Coumarin Linked Fluoroquinolones, Phthalimides and Naphthalimides as Potential DNA Gyrase Inhibitors
Letters in Drug Design & Discovery Second-Line Antiretroviral Therapy for HIV-Infected Children in Resource Limited Settings
Current Pediatric Reviews Pharmacophore Modeling Methods in Focused Library Selection – Applications in the Context of a New Classification Scheme
Combinatorial Chemistry & High Throughput Screening Assessing and Treating Cognitive Impairment in Schizophrenia: Current and Future
Current Pharmaceutical Design