6737-62-8Relevant academic research and scientific papers
Design, synthesis, anticancer, antibacterial, and antifungal evaluation of 4-aminoquinoline-1,3,5-triazine derivatives
Bhat, Hans Raj,Ghosh, Surajit Kumar,Masih, Anup,Shakya, Anshul,Singh, Udaya Pratap
, (2019/12/27)
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.
Bistriazine-based streptocyanines. Preparation, structural determination and optoelectronic properties
León, Fernando,Elizalde, Patricia,Prieto, Pilar,Sánchez-Migallón, Ana,Rodríguez, Antonio M.,De La Hoz, Antonio
, p. 307 - 319 (2016/05/09)
A series of bistriazine-based streptocyanines has been selectively prepared. A variety of substituents has been introduced into the triazine ring with p-phenylenediamine as a conjugated spacer between the triazine and the streptocyanine moieties. Fukui in
Cardioprotective effect of novel sulphonamides-1,3,5-triazine conjugates against ischaemic–reperfusion injury via selective inhibition of MMP-9
Zheng, Xiao-Zhu,Zhou, Jia-Li,Ye, Jing,Guo, Pei-Pei,Lin, Chun-Shui
, p. 756 - 765 (2016/10/19)
Diseases affecting cardiovascular system are ranked as a top most cause of morbidity and mortality. Herein, a novel class sulphonamides-1,3,5-triazine conjugates have been synthesized and tested for inhibitory activity against MMP-2 and MMP-9. The results of the study showed that these molecules efficiently inhibit MMP-9 than MMP-2, revealing compound 8e as the most potent inhibitor (IC50?=?2.34?±?0.56?nm). Due to involvement of MMP-9 in many cardiovascular diseases, particularly in myocardial ischaemia (MI), compound 8e was further subjected for the determination of the protective effect on isoproterenol (ISO)-induced myocardial injury in rats.
Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisinin-triazine hybrids and hybrid-dimers
Cloete, Theunis T.,De Kock, Carmen,Smith, Peter J.,N'Da, David D.
, p. 470 - 481 (2014/03/21)
A series of artemisinin-triazine hybrids and hybrid-dimers were synthesized and their in vitro antimalarial activity against the chloroquine sensitive (CQS), the gametocytocidal (NF54) and the choroquine resistant (CQR) Dd2 strains of Plasmodium falciparu
Antimalarial activity and docking studies of novel bi-functional hybrids derived from 4-aminoquinoline and 1,3,5-triazine against wild and mutant malaria parasites as pf-DHFR inhibitor
Bhat, Hans Raj,Singh, Udaya Pratap,Gahtori, Prashant,Ghosh, Surajit Kumar,Gogoi, Kabita,Prakash, Anil,Singh, Ramendra K.
, p. 2942 - 2952 (2013/05/08)
Bi-functional conjugates comprised of 4-aminoquinoline and 1,3,5-triazine were synthesized through facile synthetic routes. These compounds were rigorously screened for determination of their antimalarial activity against wild and mutant cultured Plasmodium falciparum. The results disclosed that the conjugates have considerable antimalarial activity against both wild and mutant parasites with marked variation on changing the pattern of substitutions. The observed activity profiles were additionally substantiated by docking studies on both wild and quadruple mutant P. falciparum dihydrofolate reductase thymidylate synthase (pf-DHFR-TS).
4-Aminoquinoline-1,3,5-triazine: Design, synthesis, in vitro antimalarial activity and docking studies
Bhat, Hans Raj,Singh, Udaya Pratap,Gahtori, Prashant,Ghosh, Surajit Kumar,Gogoi, Kabita,Prakash, Anil,Singh, Ramendra K.
, p. 2654 - 2662 (2013/09/12)
A series of hybrid 4-aminoquinoline 1,3,5-triazine derivatives was synthesized and their chemical structure were confirmed by 1H-NMR, 13C-NMR, FT-IR and mass spectrometric analyses. In vitro antimalarial activity of these compounds was evaluated against chloroquine-sensitive (3D-7) and chloroquine resistant (RKL-2) strains of P. falciparum. Results showed that all compounds had considerable antimalarial activity against both the strains and further docking studies were performed on both wild type (1J3I.pdb) and quadruple mutant (N51I, C59R, S108 N, I164L, 3QG2.pdb) pf-DHFR-TS to quantify the structural parameter necessary for the activity.
Synthesis, antimicrobial, insecticidal and anthelmintic activity studies of some new alkyl/aryl 6-(4-(4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl amino)phenyl)-N2,N4-bis(4-methoxyphenyl)-1,3,5-triazin-2, 4-diamine carbamic acid ester de
Gautam, Nidhi,Chourasia
experimental part, p. 1020 - 1026 (2012/10/08)
New carbamic acid ester derivatives containing 1,2,3-triazole nucleus have been synthesized and their antimicrobial, insecticidal and anthelmintic activity investigated. 6-(4-(4-Methyl-1H-5-carbonyl azide-1,2,3-triazol-1-yl)phenyl amino)phenyl-N2/su
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 R.,Singh, Udaya P.
, p. 598 - 604 (2012/11/07)
Some hybrid 1,3,4-thiadiazole-1,3,5-triazine derivatives tethered via -S- bridge were synthesized and characterized with the aid of spectroscopic and elemental analysis. These hybrid conjugates were then investigated for their antibacterial activity against selected Gram-positive and Gram-negative bacteria. Excellent to moderate antibacterial activity was presented by the target compounds.
Synthesis, characterization, antimicrobial, insecticidal and anthelmintic screening of some new s-triazine derivatives of pyrazoline, pyrimidine, isoxazoline and isothiazoline moiety
Gautam, Nidhi,Chourasia
, p. 1400 - 1410 (2012/11/13)
1-(4-(4,6-Bis(4′-chlorophenylamino)-1,3,5-triazin-2-ylamino)-phenyl) -3-(aryl substituted) prop-2-en-1-one 3 has been used as precursor to synthesize some new pyrimidine, pyrazoline, isoxazoline and isothiazoline derivatives. Several derivatives have been
An efficient, "green" approach to aryl amination of cyanuric chloride using acetic acid as solvent
Kolmakov, Kirill A.
, p. 533 - 539 (2008/09/18)
(Chemical Equation Presented) Acetic acid is an inexpensive and environmentally friendly solvent for facile, clean and high-yielding aryl amination of cyanuric chloride with aromatic amines, including nitroanilines. Aryl animation in acetic acid medium and isolation protocol are greatly simplified as compared to previously reported procedures. Under proper conditions, it is possible to attach the same or different aniline residues in a controlled way to obtain in excellent yields symmetrical and unsymmetrical 1,3,5-triazine derivatives, respectively.
