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
-
Respiratory Viruses, Eosinophil Activation, and Early Allergen Sensitization - Early Life Predictors of Persistent Wheezing and Asthma
Current Pediatric Reviews Heterotrimeric G Proteins Control Diverse Pathways of Transmembrane Signaling, a Base for Drug Discovery
Mini-Reviews in Medicinal Chemistry Nicotinic Receptors as Therapeutic Targets for Drug Addictive Disorders
CNS & Neurological Disorders - Drug Targets A New Aspect of the TrkB Signaling Pathway in Neural Plasticity
Current Neuropharmacology Hypersensitivity to Aurora Kinase Inhibitors in Cells Resistant against Platinum- Containing Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry High Fat Diet-Induced Obesity Stimulate Depressive Behavior in Rats
Current Psychopharmacology Graphical Abstracts
Current Neuropharmacology Immunotherapy in a Natural Model of Aβ Pathogenesis: The Aging Beagle
CNS & Neurological Disorders - Drug Targets Editorial: DSM-5 and the Challenge of Understanding and Treating Adolescents
Adolescent Psychiatry Structure and Expression of Different Serum Amyloid A (SAA) Variants and their Concentration-Dependent Functions During Host Insults
Current Medicinal Chemistry Genetic Markers in Biological Fluids for Aging-Related Major Neurocognitive Disorder
Current Alzheimer Research Natural Resins and Bioactive Natural Products thereof as Potential Anitimicrobial Agents
Current Pharmaceutical Design Endocannabinoid System: Emerging Role from Neurodevelopment to Neurodegeneration
Mini-Reviews in Medicinal Chemistry L-DOPA and Serotonergic Neurons: Functional Implication and Therapeutic Perspectives in Parkinson's Disease
Central Nervous System Agents in Medicinal Chemistry Markers of Individual Drug Metabolism: Towards the Development of a Personalized Antidepressant Prescription
Current Drug Metabolism Mechanisms of Brain Signaling During Sepsis
Current Neuropharmacology Ribosome Inactivating Proteins (RIPs) from Momordica charantia for Anti Viral Therapy
Current Molecular Medicine NGF and BDNF Alterations by Prenatal Alcohol Exposure
Current Neuropharmacology Neuroprotective Effects of Tetracyclines: Molecular Targets, Animal Models and Human Disease
CNS & Neurological Disorders - Drug Targets Leukocyte Function-Associated Antigen-1: Structure, Function and Application Prospects
Protein & Peptide Letters