37469-24-2Relevant academic research and scientific papers
Synthesis, characterization, DFT and TD-DFT study of novel bis(5,6-diphenyl-1,2,4-triazines)
Abou Kana, Maram T. H.,Ebeid, El-Zeiny M.,El-Daly, Samy A.,Elwahy, Ahmed H. M.,Mohamed, Adel A.,Sakr, Mahmoud A. S.
, (2021)
Due to the numerous biological as well as pharmacological activities of 1,2,4-triazine derivatives, we reported a synthesis of novel series of bis(5,6-diphenyl-1,2,4-triazines) via alkylation of 5,6-diphenyl-1,2,4-triazine-3(4H)-thione with the appropriate bis(halo) compounds in ethanolic KOH. The chemical structures of these compounds were confirmed by spectroscopic techniques. The absorption and excited-emission spectra of the studied novel series were monitored experimentally in ethanol solvent. The molecular structures of these triazines were optimized using B3LYP/6–31G(d) level of theory. The electronic absorption and emission spectra of the novel compounds, in gas and ethanol solvent, were calculated using time dependent density functional theory (TDDFT) at mPW1PW91/ 6–31 G (d) level. The obtained theoretical results were compared to experimental ones. The results show that, the computational optical properties of the studied novel series are in agreement with experimental results.
Diphenyl triazine hybrids inhibit α-synuclein fibrillogenesis: Design, synthesis and in vitro efficacy studies
Maqbool, Mudasir,Gadhavi, Joshna,Hivare, Pravin,Gupta, Sharad,Hoda, Nasimul
, (2020)
Aggregation of α-synuclein (α-syn) is one of the central hypotheses for Parkinson's disease (PD), therefore, its inhibition and disaggregation is an optimistic approach for the treatment of PD. Here, we report design, synthesis and in-vitro efficacy studi
Synthesis of novel 4-thiazolidinones linked by an aryl spacer to a 1,2,4-triazine moiety
Thabet, Hamdy Khamees,Ubeid, Mustafa Turki,El-Feky, Said Ahmed
, p. 567 - 573 (2015)
A series of potentially biologically active hydrazones, Schiff's base and hybrid thiazolidine-triazine derivatives have been prepared from 4-[(5,6-diphenyl-1,2,4-triazin-3-yl)thio]-benzaldehyde. The latter was prepared by reacting 5,6-diphenyl-1,2,4-triaz
Synthesis and screening of (E)-3-(2-benzylidenehydrazinyl)-5,6-diphenyl-1,2,4-triazine analogs as novel dual inhibitors of α-amylase and α-glucosidase
Alhowail, Ahmad,Ali, Muhammad,Chigurupati, Sridevi,Khan, Khalid Mohammed,Perveen, Shahnaz,Salar, Uzma,Shamim, Shahbaz,Taha, Muhammad,Ullah, Nisar,Ur Rehman, Ashfaq,Wadood, Abdul
, (2020/06/22)
(E)-3-(2-Benzylidenehydrazinyl)-5,6-diphenyl-1,2,4-triazines analogs 1–27 were synthesized by multi-step reaction scheme and subjected to in vitro inhibitory screening against α-amylase and α-glucosidase enzymes. Out of these twenty-seven synthetic analog
Multi-target inhibitors against Alzheimer disease derived from 3-hydrazinyl 1,2,4-triazine scaffold containing pendant phenoxy methyl-1,2,3-triazole: Design, synthesis and biological evaluation
Yazdani, Mahnaz,Edraki, Najmeh,Badri, Rashid,Khoshneviszadeh, Mehdi,Iraji, Aida,Firuzi, Omidreza
, p. 363 - 371 (2018/12/11)
Alzheimer's disease (AD) is a complex neurological disorder with diverse underlying pathological processes. Several lines of evidence suggest that BACE1 is a key enzyme in the pathogenesis of AD and its inhibition is of particular importance in AD treatme
Pentadienone compound containing triazine, and preparation method and application of pentadienone compound
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Paragraph 0075; 0079-0080, (2019/09/17)
The invention relates to a pentadienone compound containing triazine, and a preparation method and an application of the pentadienone compound. The compound is shown as formula A as shown in the specification. X selected from O; R is phenyl, substituted phenyl or substituted heterocyclyl; R1 is a hydrogen atom or methoxyl; and R2 is phenyl, substituted phenyl or C1-C6 alkyl. The compound has a better prevention and control effect on pseudomonas solanacearum, xanthomonas citri and xanthomonas campestris pv. oryzae.
Chalcone derivatives containing 1,2,4-triazine and production method and application thereof
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Paragraph 0035, (2019/07/04)
The invention discloses chalcone derivatives containing 1,2,4-triazine and a production method and application thereof. A general formula of the chalcone derivatives containing the 1,2,4-triazine is as shown in the description, wherein n=2,3,4, R is pheny
Novel chalcone derivatives containing a 1,2,4-triazine moiety: Design, synthesis, antibacterial and antiviral activities
Tang, Xu,Su, Shijun,Chen, Mei,He, Jun,Xia, Rongjiao,Guo, Tao,Chen, Ying,Zhang, Cheng,Wang, Jun,Xue, Wei
, p. 6011 - 6020 (2019/03/12)
A series of novel chalcone derivatives containing the 1,2,4-triazine moiety were synthesized and their structures were confirmed by 1H NMR, 13C NMR and elemental analyses. Antiviral bioassays revealed that most of the compounds exhibited good antiviral activity against tobacco mosaic virus (TMV) at a concentration of 500 μg mL-1. The designated compound 4l was 50% effective in terms of curative and protective activities against TMV with 50% effective concentrations (EC50) of 10.9 and 79.4 μg mL-1, which were better than those of ningnanmycin (81.4 and 82.2 μg mL-1). Microscale thermophoresis (MST) also showed that the binding of compound 4l to coat protein (TMV-CP) yielded a Kd value of 0.275 ± 0.160 μmol L-1, which was better than that of ningnanmycin (0.523 ± 0.250 μmol L-1). At the same time, molecular docking studies for 4l with TMV-CP (PDB code:1EI7) showed that the compound was embedded well in the pocket between the two subunits of TMV-CP. Meanwhile, compound 4a demonstrated excellent antibacterial activities against Ralstonia solanacearum (R. solanacearum), with an EC50 value of 0.1 μg mL-1, which was better than that of thiodiazole-copper (36.1 μg mL-1) and bismerthiazol (49.5 μg mL-1). The compounds act by causing folding and deformation of the bacterial cell membrane as observed using scanning electron microscopy (SEM). The chalcone derivatives thus synthesized could become potential alternative templates for novel antiviral and antibacterial agents.
Synthesis, anti-proliferative evaluation, and molecular docking studies of 3-(Alkylthio)-5,6-diaryl-1,2,4-triazines as tubulin polymerization inhibitors
Saravani, Farhad,Moghadam, Ebrahim Saeedian,Salehabadi, Hafezeh,Ostad, Seyednasser,Hamedani, Morteza Pirali,Amanlou, Massoud,Faramarzi, Mohammad Ali,Amini, Mohsen
, p. 1194 - 1201 (2019/11/22)
Background: The role of microtubules in cell division and signaling, intercellular transport, and mitosis has been well known. Hence, they have been targeted for several anti-cancer drugs. Methods: A series of 3-(alkylthio)-5,6-diphenyl-1,2,4-triazines were prepared and evaluated for their cytotoxic activities in vitro against three human cancer cell lines; human colon carcinoma cells HT-29, human breast adenocarcinoma cell line MCF-7, human Caucasian gastric adenocarcinoma cell line AGS as well as fibroblast cell line NIH-3T3 by MTT assay. Docking simulation was performed to insert these compounds into the crystal structure of tubulin at the colchicine binding site to determine a probable binding model. Compound 5d as the most active compound was selected for studying of microtubule disruption. Results: Compound 5d showed potent cytotoxic activity against all cell lines. The molecular modeling study revealed that some derivatives of triazine strongly bind to colchicine binding site. The tubulin polymerization assay kit showed that the cytotoxic activity of 5d may be related to inhibition of tubulin polymerization. Conclusion: The cytotoxicity and molecular modeling study of the synthesized compounds with their inhibition activity in tubulin polymerization demonstrate the potential of triazine derivatives for development of new anti-cancer agents.
COMPOSITIONS AND METHODS FOR REDUCING CELL VIABILITY
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Paragraph 0065; 0067; 0192-0193, (2019/11/11)
This invention is directed to compositions, methods and kits that can be used for reducing cell viability, inducing cell apoptosis, and inhibiting cell proliferation, such as for the treatment of cancer. The invention is also directed to compositions, met
