Abstract
Some alkylthio, alkylsulfinyl and alkylsulfonyl-5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles were synthesized and evaluated against Helicobacter pylori. The antibacterial data indicated that most compounds exhibited significant inhibitory activity against H. pylori- more potent than standard drug metronidazole. Among them, 2-ethylsulfinyl-5-(5-nitro-2- thienyl)-1,3,4-thiadiazole was the most potent compound tested against clinical isolates of H. pylori. Generally the SAR of this series of compounds indicated that both the structure of the alkyl pendent and the S, SO or SO2 linker dramatically impact the antibacterial activity against H. pylori.
Keywords: Antibacterial activity, Anti-Helicobacter pylori activity, 1,3,4-Thiadiazole, Nitrothiophene
Letters in Drug Design & Discovery
Title: Synthesis and Structure-Activity Relationship Study of 2-Substituted- 5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles as Anti-Helicobacter pylori Agents
Volume: 6 Issue: 6
Author(s): Alireza Foroumadi, Somayeh Sedaghat, Saeed Emami, Maryam Yazdanian, Mohammad Hassan Moshafi, Maliheh Safavi, Amirhossein Sakhteman, Loghman Firoozpour, Mohsen Vosooghi and Abbas Shafiee
Affiliation:
Keywords: Antibacterial activity, Anti-Helicobacter pylori activity, 1,3,4-Thiadiazole, Nitrothiophene
Abstract: Some alkylthio, alkylsulfinyl and alkylsulfonyl-5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles were synthesized and evaluated against Helicobacter pylori. The antibacterial data indicated that most compounds exhibited significant inhibitory activity against H. pylori- more potent than standard drug metronidazole. Among them, 2-ethylsulfinyl-5-(5-nitro-2- thienyl)-1,3,4-thiadiazole was the most potent compound tested against clinical isolates of H. pylori. Generally the SAR of this series of compounds indicated that both the structure of the alkyl pendent and the S, SO or SO2 linker dramatically impact the antibacterial activity against H. pylori.
Export Options
About this article
Cite this article as:
Foroumadi Alireza, Sedaghat Somayeh, Emami Saeed, Yazdanian Maryam, Moshafi Hassan Mohammad, Safavi Maliheh, Sakhteman Amirhossein, Firoozpour Loghman, Vosooghi Mohsen and Shafiee Abbas, Synthesis and Structure-Activity Relationship Study of 2-Substituted- 5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles as Anti-Helicobacter pylori Agents, Letters in Drug Design & Discovery 2009; 6 (6) . https://dx.doi.org/10.2174/157018009789057599
DOI https://dx.doi.org/10.2174/157018009789057599 |
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
-
A Review of the Effects of Hypoxia, Sleep Deprivation and Transcranial Magnetic Stimulation on EEG Activity in Humans: Challenges for Drug Discovery for Alzheimer's Disease
Current Alzheimer Research The Role of IRE1 Signaling in the Central Nervous System Diseases
Current Neuropharmacology Current Indications for Implantable Cardioverter Defibrillators in Non-Ischemic Cardiomyopathies and Channelopathies
Reviews on Recent Clinical Trials Neuroprotective Polyphenols: A Modulatory Action on Neurotransmitter Pathways
Current Neuropharmacology Physiotherapy for Ankylosing Spondylitis: Systematic Review and a Proposed Rehabilitation Protocol
Current Rheumatology Reviews Errors in ADAS-Cog Administration and Scoring May Undermine Clinical Trials Results
Current Alzheimer Research Chemical Constituents of Plants from the Genus Valeriana
Mini-Reviews in Organic Chemistry Novel Dibenzothiepins with Antibiofilm Activity Demonstrated by Microbiological Assays and Molecular Modeling
Current Organic Chemistry Meet Our Editorial Board Member
CNS & Neurological Disorders - Drug Targets The Effect of Sodium Metabisulphite on Apoptosis in the Experimental Model of Parkinson’s Disease
Current Nutrition & Food Science Microbial Genomics and Novel Antibiotic Discovery: New Technology to Search for New Drugs
Current Pharmaceutical Design Managing Erectile Dysfunction in Heart Failure
Endocrine, Metabolic & Immune Disorders - Drug Targets The Heart and Brain Imaging in Lone Atrial Fibrillation – Are We Surprised?
Current Pharmaceutical Design QSAR Analysis of Compounds Exhibiting General Anesthetics’ Properties
Letters in Drug Design & Discovery An Historical Perspective on Efforts to Treat Transmissible Spongiform Encephalopathy
CNS & Neurological Disorders - Drug Targets Modulation of Monoaminergic Transporters by Choline-Containing Phospholipids in Rat Brain
CNS & Neurological Disorders - Drug Targets A PHACES Syndrome Unmasked by Propranolol Interruption in a Tetralogy of Fallot Patient: Case Report and Extensive Review on New Indications of Beta Blockers
Current Medicinal Chemistry Problematic Internet Use, Sleep Quality and Academic Achievement In Turkish University Students
Adolescent Psychiatry Designing of Selective γ-Secretase Inhibitory Benzenesulfonamides through Comparative In Vitro and In Silico Analysis
Current Drug Discovery Technologies Editorial: Speech Production in Persons with Dementia
Current Alzheimer Research