Design, Facile Synthesis, and Antibacterial Activity of Hybrid 1,3,4‐thiadiazole‐1,3,5‐triazine Derivatives Tethered via –S– Bridge

Dubey, Vaibhav; Pathak, Manish; Bhat, Hans Raj; Singh, Udaya Pratap

doi:10.1111/j.1747-0285.2012.01433.x

Cited by 49 publications

(24 citation statements)

References 17 publications

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“…Heterocyclic molecules are well known for their importance in medicinal chemistry because of diverse pharmacological benefits and ease of derivatization for the generation of newer scaffolds . In this regard, 4‐aminoquinoline and 1,3,5‐triazine have gained a lot of attention from the researchers because of an extensive array of pharmacological properties, such as antibacterial, antimalarial, anti‐inflammatory, antifungal, anti‐HIV, anti‐diabetic, and against cystic fibrosis . More recently, these pharmacophores showed excellent anticancer activity .…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, anticancer, antibacterial, and antifungal evaluation of 4‐aminoquinoline‐1,3,5‐triazine derivatives

Bhat

Masih

Shakya

et al. 2019

Journal of Heterocyclic Chem

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A series of 4-aminoquinoline 1,3,5-triazine derivatives were synthesized and evaluated for anticancer activity against cancer cell lines HeLa, MCF-7, HL-60, HepG2 where these derivatives exert significant anticancer activity. The molecules found nontoxic against MCF-12A. The molecules also showed potent inhibition of EGFR-TK as compared to eroltinib in enzyme-based assay. The newly synthesized derivatives were screened for their in vitro antibacterial and antifungal activity against Bacillus subtilis, Bacillus cereus, Staphylococcus aureus, Proteus vulgaris, Escherichia coli, Pseudomonas aeruginosa and Candida albicans, Aspergillus niger, Aspergillus fumigatus using cefixime and fluconazole as standard. Antibacterial screening results suggest that compound 7c showed potent activity against S. aureus, P. aeruginosa, and P. vulgaris. In antifungal screening, compound 7b showed significant activity against A. niger, A. fumigatus and moderate activity against C. albicans. NaHCO 3 (iii) KSCN, 1,4 dioxane, reflux at 105 C for 7-8 hours, K 2 CO 3 , tin granules (iv) dry acetone, reflux for 10-11 hours at 60-65 C PHARMACOLOGICAL ACTIVITY OF 4-AMINOQUINOLINE 1,3,5-TRIAZINES DERIVATIVES 391

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Section: Introductionmentioning

confidence: 99%

Design, synthesis, anticancer, antibacterial, and antifungal evaluation of 4‐aminoquinoline‐1,3,5‐triazine derivatives

Bhat

Masih

Shakya

et al. 2019

Journal of Heterocyclic Chem

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“…In this regard, derivatives of 1,3,5‐triazine have received considerable attention . 1,3,5‐Triazines have various pharmacological activities, such as antibacterial, antifungal, antimalarial, antidiabetic and anticystic fibrosis effects. Moreover, 1,3,5‐triazine exerts anticancer effects by inhibiting PI3K/mTOR, Rad6 ubiquitin conjugating enzyme and human epidermal growth factor receptor tyrosine kinases (EGFR‐TKs) …”

Section: Introductionmentioning

confidence: 99%

Novel 1,3,5‐triazine derivatives exert potent anti‐cervical cancer effects by modulating Bax, Bcl2 and Caspases expression

Wang

et al. 2017

Chem Biol Drug Des

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This study aimed to develop novel 1,3,5-triazine derivatives as potent anti-cervical cancer agents. The compounds were synthesized in short steps with an excellent yield and characterized via various spectroscopic and analytical methods. A structure-activity relationship study suggested that electron-withdrawing substituents showed greater anticancer activity than electron-donating groups. Compound 7p (p-fluoro) showed the highest activity against cervical cancer cells. In a nude mouse xenograft model inoculated with HeLa cells, 7p showed dose-dependent inhibition of cervical tumour growth. Histopathological examination of excised tumour-bearing tissues showed that 7p improved the microstructure in a dose-dependent manner. Compound 7p also increased the proportions of HeLa cells in G0/G1 and S-phase and significantly decreased that of G2/M-phase. The effects of 7p on C-caspase-3, C-caspase-9, Bcl-2 and Bax expression in HeLa cells were also determined.

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“…Concerning the immense pharmacological activity of 1,3,5‐triazine and in follow up of our previous studies toward the development of novel antibacterial compounds derived from 1,3,5‐triazine, here we wish to report a novel class of hybrid 4‐aminoquinoline 1,3,5‐triazine .…”

Section: Introductionmentioning

confidence: 99%

Hybrid 4‐Aminoquinoline‐1,3,5‐triazine Derivatives: Design, Synthesis, Characterization, and Antibacterial Evaluation

Pathak

Thakur

Bhat

et al. 2014

Journal of Heterocyclic Chem

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A series of novel 4‐aminoquinoline 1,3,5‐triazine derivatives were synthesized and characterized by FTIR, 1H‐NMR, 13C‐NMR, MS, and elemental analysis. The antibacterial activities of synthesized compounds were tested against three Gram‐positive bacteria, namely Bacillus subtilis (NCIM‐2063), Bacillus cereus (NCIM‐2156), and Staphylococcus aureus (NCIM‐2079), and four Gram‐negative bacteria, namely Proteus vulgaris (NCIM‐2027), Proteus mirabilis (NCIM‐2241), Escherichia coli (NCIM‐2065), and Pseudomonas aeruginosa (NCIM‐2036), using ciprofloxacin as reference standard drug. Results showed compound 9a and 9e as potent antibacterial agents against all bacterial strains except Bacillus cereus (NCIM‐2156). Copyright © 2014 HeteroCorporation

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Design, Facile Synthesis, and Antibacterial Activity of Hybrid 1,3,4‐thiadiazole‐1,3,5‐triazine Derivatives Tethered via –S– Bridge

Cited by 49 publications

References 17 publications

Design, synthesis, anticancer, antibacterial, and antifungal evaluation of 4‐aminoquinoline‐1,3,5‐triazine derivatives

Design, synthesis, anticancer, antibacterial, and antifungal evaluation of 4‐aminoquinoline‐1,3,5‐triazine derivatives

Novel 1,3,5‐triazine derivatives exert potent anti‐cervical cancer effects by modulating Bax, Bcl2 and Caspases expression

Hybrid 4‐Aminoquinoline‐1,3,5‐triazine Derivatives: Design, Synthesis, Characterization, and Antibacterial Evaluation

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