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.
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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 |
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