2394-87-8Relevant academic research and scientific papers
Heterocyclic IDH mutant inhibitor, preparation method and application thereof
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Paragraph 0102-0107; 0263; 0266-0268, (2020/09/23)
The invention discloses a heterocyclic IDH mutant inhibitor, a preparation method and application thereof, belongs to the field of medicines, and particularly relates to a s-triazine compound with structural characteristics of a general formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition, a preparation method of the s-triazine compound, and application of the s-triazine compound or the pharmaceutically acceptable salt and the pharmaceutical composition as isocitrate dehydrogenase 2 (IDH2) mutant inhibitors. The compound disclosed by the invention has an obvious inhibiting effect on the activity of an IDH2 mutant (mIDH2), can effectively inhibit the process of catalyzing alpha-ketoglutaric acid to generate 2-hydroxyglutaric acid by the mIDH2, and can be used for preventing and/or treating various related diseases including cancers caused by IDH2 mutation.
Triazine compound as well as preparation method and application thereof
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Paragraph 0027; 0028; 0029; 0126; 0127; 0128, (2017/11/30)
The invention provides a triazine compound shown as a chemical formula (I) and a preparation method thereof as well as an application of the triazine compound in preparing drugs for treating central nervous system diseases. In the formula, R1 is selected
De novo lead optimization of triazine derivatives identifies potent antimalarials
Shandilya, Ashutosh,Hoda, Nasimul,Khan, Sameena,Jameel, Ehtesham,Kumar, Jitendra,Jayaram
, p. 96 - 103 (2016/11/25)
Malaria is a life-threatening disease caused by Plasmodium parasites among which Plasmodium falciparum is the most deadly. Due to the widespread resistance of the current antimalarial drugs, intense research efforts are focused on identification of new an
Rational design, synthesis and biological screening of triazine-triazolopyrimidine hybrids as multitarget anti-Alzheimer agents
Jameel, Ehtesham,Meena, Poonam,Maqbool, Mudasir,Kumar, Jitendra,Ahmed, Waqar,Mumtazuddin, Syed,Tiwari, Manisha,Hoda, Nasimul,Jayaram
, p. 36 - 51 (2017/05/09)
In our endeavor towards the development of potent multitarget ligands for the treatment of Alzheimer's disease, a series of triazine-triazolopyrimidine hybrids were designed, synthesized and characterized by various spectral techniques. Docking and scoring techniques were used to design the inhibitors and to display their interaction with key residues of active site. Organic synthesis relied upon convergent synthetic routes were mono and di-substituted triazines were connected with triazolopyrimidine using piperazine as a linker. In total, seventeen compounds were synthesized in which the di-substituted triazine-triazolopyrimidine derivatives 9a-d showed better acetylcholinesterase (AChE) inhibitory activity than the corresponding tri-substituted triazine-triazolopyrimidine derivatives 10a-f. Out of the disubstituted triazine-triazolopyrimidine based compounds, 9a and 9b showed encouraging inhibitory activity on AChE with IC50 values 0.065 and 0.092?μM, respectively. Interestingly, 9a and 9b also demonstrated good inhibition selectivity towards AChE over BuChE by ~28 folds. Furthermore, kinetic analysis and molecular modeling studies showed that 9a and 9b target both catalytic active site as well as peripheral anionic site of AChE. In addition, these derivatives effectively modulated Aβ self-aggregation as investigated through CD spectroscopy, ThT fluorescence assay and electron microscopy. Besides, these compounds exhibited potential antioxidants (2.15 and 2.91 trolox equivalent by ORAC assay) and metal chelating properties. In silico ADMET profiling highlighted that, these novel triazine derivatives have appropriate drug like properties and possess very low toxic effects in the primarily pharmacokinetic study. Overall, the multitarget profile exerted by these novel triazine molecules qualified them as potential anti-Alzheimer drug candidates in AD therapy.
Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents
Maqbool, Mudasir,Manral, Apra,Jameel, Ehtesham,Kumar, Jitendra,Saini, Vikas,Shandilya, Ashutosh,Tiwari, Manisha,Hoda, Nasimul,Jayaram
, p. 2777 - 2788 (2016/06/08)
A series of new cyanopyridine-triazine hybrids were designed, synthesized and screened as multitargeted anti-Alzheimer's agents. These molecules were designed while using computational techniques and were synthesized via a feasible concurrent synthetic ro
In vitro antimycobacterial and antimicrobial activity of some new pyrazoline, isoxazole and benzodiazepine derivatives containing 1,3,5-triazine nucleus via chalcone series
Solankee, Anjani,Tailor, Riki,Kapadia, Kishor
, p. 1277 - 1287 (2017/04/28)
In the present study, three new combinatorial libraries of substituted phenyl pyrazoline 5a-e, isoxazole 6a-e and 1,5-benzodiazepine 7a-e derivatives have been synthesised via the reaction of chalcone 4a-e with Phenylhydrazine hydrochloride, hydroxylamine
Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-Diamino-piperidinyl triazines
Zhou, Yuefen,Sun, Zhongxiang,Froelich, Jamie M.,Hermann, Thomas,Wall, Daniel
, p. 5451 - 5456 (2007/10/03)
Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole cell antibacterial activity was achieved by linking additional aromatic moieties at the triazine C-4 position.
