Synthesis and biological evaluation of novel 2,4,6-triazine derivatives as antimicrobial agents

Gavade, Sandip N.; Markad, Vijay L.; Kodam, Kisan M.; Shingare, Murlidhar S.; Mane, Dhananjay V.

doi:10.1016/j.bmcl.2012.05.111

Cited by 31 publications

(16 citation statements)

References 25 publications

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“…TCT is an attractive linker due to its low cost, commercial availability, and ease of stepwise substitution of the three chlorine atoms (Blotny, 2006 ). TCT derivatives are known to exhibit a broad range of biological activities, including anti-bacterial (Solankee et al, 2010 ; Gavade et al, 2012 ; Patel et al, 2012 ), anti-fungal (Singh et al, 2012 ), anti-cancer (Brzozowski and Saczewski, 2002 ; Zhu et al, 2012 ; Kumar et al, 2013 ), anti-malarial (Kumar et al, 2009 ; Sunduru et al, 2010 ), anti-TB (Sunduru et al, 2010 ; Avupati et al, 2013 ), as well as herbicidal effects (Zhao et al, 2011 ) etc. Several research groups have also explored the application of TCT in solid phase synthesis by means of a combinatorial approach (Masala and Taddei, 1999 ) for the synthesis of dendrimers (Simanek et al, 2009 , 2013 ; Lim et al, 2012 ) and non-covalently bound supra-molecular aggregates (Lehn et al, 1990 ; Mathias et al, 1994 ; Timmerman et al, 1997 ; Timmerman and Prins, 2001 ).…”

Section: Introductionmentioning

confidence: 99%

Exploring the Orthogonal Chemoselectivity of 2,4,6-Trichloro-1,3,5-Triazine (TCT) as a Trifunctional Linker With Different Nucleophiles: Rules of the Game

et al. 2018

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Section: Introductionmentioning

confidence: 99%

Exploring the Orthogonal Chemoselectivity of 2,4,6-Trichloro-1,3,5-Triazine (TCT) as a Trifunctional Linker With Different Nucleophiles: Rules of the Game

et al. 2018

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“…The need for effective therapies against multidrug-resistant bacterial strains has stimulated research into the design and synthesis of novel antimicrobial molecules. [5] Diarylsulfonylureas are the structural analogs of urea (NH 2 CONH 2 ) with aromatic sulfonyl group in the position 3 and an aromatic or heteroaromatic ring at the position 1. Diarylsulfonylureas became widely available since 1955 as popular antidiabetic drugs in clinical practice for the treatment of type 2 diabetes, by virtue of their insulin secretagogue properties.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Naidu¹

2018

AJP

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Introduction:To study the antimicrobial effect of novel diarylsulfonylurea-chalcone hybrids with significant associated morbidity and mortality which is mainly due to the development of microbial resistance to the existing antimicrobial agents. Materials and Methods: The antimicrobial effect of novel diarylsulfonylurea-chalcone hybrid molecules was evaluated by agar well diffusion method against various strains of bacteria and fungi. Results: Most of the compounds showed promising antibacterial and antifungal activity. Conclusion: The results in the present study suggest that novel diarylsulfonylurea-chalcone hybrids can be used in treating diseases caused by the tested organisms.

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“…These compounds exhibit antimalarial [ 9 – 16 ], antimicrobial [ 17 – 25 ], anti-cancer [ 26 – 31 ] and anti-viral activities [ 32 ], among other beneficial properties. On the other hand, treatment of bacterial infections remains a challenging therapeutic problem because of emerging infectious diseases and the increasing number of multidrug-resistant microbial pathogens [ 33 ]. As multidrug-resistant bacterial strains proliferate, the necessity for effective therapy has stimulated research into the design and synthesis of novel antimicrobial molecules [ 34 – 42 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization and evaluation of 1,3,5-triazine aminobenzoic acid derivatives for their antimicrobial activity

Al‐Zaydi

Khalil

El‐Faham

et al. 2017

Chemistry Central Journal

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BackgroundReplacement of chloride ions in cyanuric chloride give several variants of 1,3,5-triazine derivatives which were investigated as biologically active small molecules. These compounds exhibit antimalarial, antimicrobial, anti-cancer and anti-viral activities, among other beneficial properties. On the other hand, treatment of bacterial infections remains a challenging therapeutic problem because of the emerging infectious diseases and the increasing number of multidrug-resistant microbial pathogens. As multidrug-resistant bacterial strains proliferate, the necessity for effective therapy has stimulated research into the design and synthesis of novel antimicrobial molecules.Results1,3,5-Triazine 4-aminobenzoic acid derivatives were prepared by conventional method or by using microwave irradiation. Using microwave irradiation gave the desired products in less time, good yield and higher purity. Esterification of the 4-aminobenzoic acid moiety afforded methyl ester analogues. The s-triazine derivatives and their methyl ester analogues were fully characterized by FT-IR, NMR (1H-NMR and 13C-NMR), mass spectra and elemental analysis. All the synthesized compounds were evaluated for their antimicrobial activity. Some tested compounds showed promising activity against Staphylococcus aureus and Escherichia coli. ConclusionsThree series of mono-, di- and trisubstituted s-triazine derivatives and their methyl ester analogues were synthesized and fully characterized. All the synthesized compounds were evaluated for their antimicrobial activity. Compounds (10), (16), (25) and (30) have antimicrobial activity against S. aureus comparable to that of ampicillin, while the activity of compound (13) is about 50% of that of ampicillin. Compounds (13) and (14) have antimicrobial activity against E. coli comparable to that of ampicillin, while the activity of compounds (9–12) and (15) is about 50% of that of ampicillin. Furthermore, minimum inhibitory concentrations values for clinical isolates of compounds (10), (13), (14), (16), (25) and (30) were measured. Compounds (10) and (13) were more active against MRSA and E. coli than ampicillin. Invitro cytotoxicity results revealed that compounds (10) and (13) were nontoxic up to 250 µg/mL (with SI = 10) and 125 µg/mL (with SI = 5), respectively.Graphical abstractThree series of mono-, di- and trisubstituted s-triazine derivatives and their methyl ester analogues were synthesized and evaluated for their antimicrobial activity. Several compounds have antimicrobial activity against S. aureus and E. coli comparable to that of ampicillin. Electronic supplementary materialThe online version of this article (doi:10.1186/s13065-017-0267-3) contains supplementary material, which is available to authorized users.

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Synthesis and biological evaluation of novel 2,4,6-triazine derivatives as antimicrobial agents

Cited by 31 publications

References 25 publications

Exploring the Orthogonal Chemoselectivity of 2,4,6-Trichloro-1,3,5-Triazine (TCT) as a Trifunctional Linker With Different Nucleophiles: Rules of the Game

Exploring the Orthogonal Chemoselectivity of 2,4,6-Trichloro-1,3,5-Triazine (TCT) as a Trifunctional Linker With Different Nucleophiles: Rules of the Game

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Synthesis, characterization and evaluation of 1,3,5-triazine aminobenzoic acid derivatives for their antimicrobial activity

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