Abstract
Due to overwhelming generation of drug resistant microorganisms, there is an urgent need to develop novel chemotherapeutic agents. In continuation of our research on discovery of novel heterocyclic scaffolds from 1,3,5-triazine, present study deals with design and development of some novel di- and tri-substituted 1,3,5-triazine derivatives. The synthesis of title analogues were accomplished by SNAr reaction and subsequently underwent rigorous antibacterial screening against a panel of representative Gram-negative and Gram-positive bacteria. Screening results revealed that minor structural variation may induce drastic changes in activity. Whereas, amine bridge and piprazine was termed as pivotal structural fragments necessary for generation and escalation of bio-activity. The structures of newly synthesized compounds were ascertained on the basis of their analytical and spectral profiles.
Keywords: 1,3,5-triazine, Synthesis, Antibacterial, Nucleophilic Substitution, FTIR spectrum, Facile Synthesis, scaffolds, P. mirabillis, Gram-negative micro-organisms, B. subtilis, E. coli, Spectroscope (LC-MS), RX-I spectroscope, S. aureus
Letters in Drug Design & Discovery
Title: Design, Facile Synthesis, Antibacterial Activity and Structure-Activity Relationship of Novel Di- and Tri-Substituted 1,3,5-Triazines
Volume: 9 Issue: 3
Author(s): Surajit Kumar Ghosh, Ashmita Saha, Bornali Hazarika, Udaya Pratap Singh, Hans Raj Bhat and Prashant Gahtori
Affiliation:
Keywords: 1,3,5-triazine, Synthesis, Antibacterial, Nucleophilic Substitution, FTIR spectrum, Facile Synthesis, scaffolds, P. mirabillis, Gram-negative micro-organisms, B. subtilis, E. coli, Spectroscope (LC-MS), RX-I spectroscope, S. aureus
Abstract: Due to overwhelming generation of drug resistant microorganisms, there is an urgent need to develop novel chemotherapeutic agents. In continuation of our research on discovery of novel heterocyclic scaffolds from 1,3,5-triazine, present study deals with design and development of some novel di- and tri-substituted 1,3,5-triazine derivatives. The synthesis of title analogues were accomplished by SNAr reaction and subsequently underwent rigorous antibacterial screening against a panel of representative Gram-negative and Gram-positive bacteria. Screening results revealed that minor structural variation may induce drastic changes in activity. Whereas, amine bridge and piprazine was termed as pivotal structural fragments necessary for generation and escalation of bio-activity. The structures of newly synthesized compounds were ascertained on the basis of their analytical and spectral profiles.
Export Options
About this article
Cite this article as:
Kumar Ghosh Surajit, Saha Ashmita, Hazarika Bornali, Pratap Singh Udaya, Raj Bhat Hans and Gahtori Prashant, Design, Facile Synthesis, Antibacterial Activity and Structure-Activity Relationship of Novel Di- and Tri-Substituted 1,3,5-Triazines, Letters in Drug Design & Discovery 2012; 9 (3) . https://dx.doi.org/10.2174/157018012799129846
DOI https://dx.doi.org/10.2174/157018012799129846 |
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
-
Generation of Human Cardiomyocytes for Cardiac Regenerative Therapies: Differentiation and Direct Reprogramming
Current Pharmaceutical Design Challenges and Perspectives in the Discovery of Dengue Virus Entry Inhibitors
Current Medicinal Chemistry The Structure and Pharmacological Functions of Coumarins and Their Derivatives
Current Medicinal Chemistry Quantitative Structure-Activity Relationship (QSAR) Analysis to Predict Drug-Drug Interactions of ABC Transporter ABCG2
Mini-Reviews in Medicinal Chemistry Luminescent G-quadruplex Probes
Current Pharmaceutical Design Novel Tricyclic Indeno[5,6-b]furan-imidazole Hybrid Compounds: Design, Synthesis and Antitumor Activity
Letters in Drug Design & Discovery Synthesis and Biological Evaluation of 2-amino-3-(3, 4, 5-trimethoxyphenylsulfonyl)-5-aryl thiophenes as a New Class of Antitubulin Agents
Medicinal Chemistry Sugar Sulfamates for Seizure Control: Discovery and Development of Topiramate, a Structurally Unique Antiepileptic Drug
Current Topics in Medicinal Chemistry Heterocycle-thioacetic Acid Motif: A Privileged Molecular Scaffold with Potent, Broad-Ranging Pharmacological Activities
Current Pharmaceutical Design Fibroblast Growth Factor Receptor Inhibitors
Current Pharmaceutical Design 1,2,5-Thiadiazole Scaffold: A Review on Recent Progress in Biological Activities
Combinatorial Chemistry & High Throughput Screening The Role of Celecoxib as a Potential Inhibitor in the Treatment of Inflammatory Diseases - A Review
Current Medicinal Chemistry Role of TREM2 in Alzheimer's Disease and its Consequences on β- Amyloid, Tau and Neurofibrillary Tangles
Current Alzheimer Research Sulfonated Organic Heteropolyacid Salts: Recyclable Green Solid Catalysts for the Highly Efficient and Green Synthesis of Bis(indolyl)methanes in Water
Letters in Organic Chemistry How to Manage the Infectious Risk under Anti-TNF in Inflammatory Bowel Disease
Current Drug Targets Advances in Drug Discovery based on Genomics, Proteomics and Bioinformatics (Part II)
Current Topics in Medicinal Chemistry Inhibition of DNA Topoisomerases by a Series of Benzoxazoles and their Possible Metabolites
Letters in Drug Design & Discovery Mass Spectrometric Identification of Collagen Alpha-1 (III) Chain and Chondroitin Sulfate Proteoglycan-4 Nitration in Patients with Acute Pulmonary Embolism
Current Proteomics Preface
Current Stem Cell Research & Therapy Chemotherapeutic Agents Against Malaria: What Next After Chloroquine?
Current Topics in Medicinal Chemistry