Design, Facile Synthesis, Antibacterial Activity and Structure-Activity Relationship of Novel Di- and Tri-Substituted 1,3,5-Triazines

Author(s): Surajit Kumar Ghosh, Ashmita Saha, Bornali Hazarika, Udaya Pratap Singh, Hans Raj Bhat, Prashant Gahtori.

Journal Name: Letters in Drug Design & Discovery

Volume 9 , Issue 3 , 2012

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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

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Article Details

Year: 2012
Page: [329 - 335]
Pages: 7
DOI: 10.2174/157018012799129846
Price: $65

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