2272-29-9Relevant academic research and scientific papers
Synthesis, chemical and biological investigations of new Ru(III) and Se(IV) complexes containing 1,3,5-triazine chelating derivatives
Al-Khodir, Fatima A.I.,Al-Warhi, Tarfah,Abumelha, Hana M.A.,Al-Issa
, p. 795 - 808 (2019)
A series of vital complexes of [Se (Ln) (Cl)x]·yCl (where n = L1, L2, L3 and L4; x = 1, 2, or 3 and y = 1, 2, or 3) and [Ru (Ln) (Cl)x (H2O)y]zCl
Discovery of Mycobacterium tuberculosis Rv3364c-Derived Small Molecules as Potential Therapeutic Agents to Target SNX9 for Sepsis
Cho, Euni,Jang, Sein,Jeon, Hye-In,Jeong, Young Jin,Kim, Hyo Keun,Kim, Kyungmin,Lee, Daeun,Lee, Eunbi,Lee, Youngbok,Lee, Yuno,Min, Sun-Joon,Mun, Seok-Jun,Oh, Ji Eun,Son, Wooic,Yang, Chul-Su,Yoo, Hye Hyun
, (2022/01/20)
The serine protease inhibitor Rv3364c of Mycobacterium tuberculosis (MTB) is highly expressed in cells during MTB exposure. In this study, we showed that the 12WLVSKF17 motif of Rv3364c interacts with the BAR domain of SNX9 and inhibits endosome trafficki
Design and development of novel thiazolidin-4-one-1,3,5-triazine derivatives as neuro-protective agent against cerebral ischemia–reperfusion injury in mice via attenuation of NF-?B
Lu, Min,Qi, Yujun,Han, Yu,Yi, Qiong,Xu, Lei,Sun, Wenlin,Ni, Guihua,Ni, Xiaoyu,Xu, Changsong
, p. 1315 - 1327 (2020/07/13)
The present study enumerates the discovery and development of novel thiazolidin-4-one-1,3,5-triazine as neuro-protective agent against cerebral ischemia–reperfusion injury in mice. These compounds showed significant inhibition of NF-?B transcriptional activity in LPS-stimulated RAW264.7 cells, displaying compound 8k as most potent inhibitor among the tested derivative. The compound 8k was further studied in in vivo middle cerebral artery occlusion (MCAO) mice model for neuro-protective action. Results suggest that compound 8k causes attenuation of inflammation (TNF-α, IL-β, and IL-6), oxidative stress (SOD, GSH, and MDA), and apoptosis (Bcl-2, Bax, and cleaved caspase-3) in MCAO mice in concentration-dependent manner. Collectively, our results documented that compound 8k pre-treatment protects cerebral I/R. This novel lead scaffold may be helpful for investigation of new neuro-protective agent by inactivation of NF-?B.
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice
Singh, Palwinder,Kaur, Sukhmeet,Kumari, Priya,Kaur, Baljit,Kaur, Manpreet,Singh, Gurjit,Bhatti, Rajbir,Bhatti, Manpreet
, p. 7929 - 7941 (2018/09/06)
Here, we report analgesic and anti-inflammatory activity of a series of compounds obtained by appending 4-aminophenylmorpholin-3-one and acyclic, cyclic, or heterocyclic moieties on 1,3,5-triazine. The structures of compounds 4b and 6b are optimized for the best inhibition of COX-2 with IC50 values of 0.06 and 0.08 μM, respectively, and selectivity over COX-1 of 166 and >125, respectively. At the dose of 5 mg kg-1, these compounds significantly reduced acetic acid induced writhings, and their ED50 values were found to be 2.2 and 1.9 mg kg-1, respectively. Besides the cell-based and animal-based experiments showing the modes of action of these compounds targeting COX-2, the interaction behavior of 4b with COX-2 was also characterized, with physicochemical experiments including ITC, NMR, UV-vis, and molecular-modeling studies. Characteristically, these compounds interact with R120, Y355, and W385, the residues responsible for holding the substrate and mediating the process of electron transfer during the metabolic phase of the enzyme.
Triazine compound as well as preparation method and application thereof
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Paragraph 0027; 0028; 0029; 0063; 0064; 0065, (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
Synthesis and Biological Evaluation of Amidinourea and Triazine Congeners as Inhibitors of MDA-MB-231 Human Breast Cancer Cell Proliferation
Bass, Rosemary,Jenkinson, Sarah,Wright, Jennifer,Smulders-Srinivasan, Tora,Marshall, Jamie C.,Castagnolo, Daniele
supporting information, p. 288 - 291 (2017/03/01)
A series of novel amidinourea derivatives was synthesized, and the compounds were evaluated as inhibitors of MDA-MB-231 human breast cancer cell proliferation. In addition, a second series of triazine derivatives designed as rigid congeners of the amidinoureas was synthesized, and the compounds were evaluated for their antiproliferative activity. Among the two series, amidinourea 3 d (N-[N-[8-[[N-(morpholine-4-carbonyl)carbamimidoyl]amino]octyl]carbamimidoyl]morpholine-4-carboxamide) emerged as a potent anticancer hit compound with an IC50value of 0.76 μm, similar to that of tamoxifen.
Elaborate ligand-based modeling and subsequent synthetic exploration unveil new nanomolar Ca2+/calmodulin-dependent protein kinase II inhibitory leads
Shahin, Rand,Taha, Mutasem O.
experimental part, p. 377 - 400 (2012/03/09)
Ca2+/calmodulin-dependent protein kinase II (CaMKII) has been recently implicated in cardiovascular diseases and hypertension prompting several attempts to discover and optimize new CaMKIIδ inhibitors. Towards this end we explored the pharmacophoric space of 88 CaMKIIδ inhibitors using nine diverse sets of inhibitors to identify high quality pharmacophores. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select an optimal combination of pharmacophoric models and 2D physicochemical descriptors capable of accessing self-consistent quantitative structure-activity relationship (QSAR) of optimal predictive potential (r722=0.70, F = 18.19, rLOO2=0.71, rPRESS2 against 16 external test inhibitors = 0.60). Three orthogonal pharmacophores emerged in the QSAR equation suggesting the existence of at least three binding modes accessible to ligands within CaMKIIδ binding pocket. Receiver operating characteristic (ROC) curves analysis established the validity of QSAR-selected pharmacophores. We employed the pharmacophoric models and associated QSAR equation to screen the national cancer institute (NCI) list of compounds. In silico screening identified nanomolar and low micromolar inhibitors. The most potent hits exhibited IC 50 values of 20 and 82 nM. The best pharmacophoric model (Hypo8/31) was employed to guide the synthesis of novel triazine-based CaMKIIδ inhibitors, of which the most potent illustrated an IC50 value of 154 nM against CaMKIIδ.
Synthesis and in vitro antibacterial screening of some new 2,4,6-trisubstituted-1,3,5-triazine derivatives
Singh, Ravi Bhushan,Das, Nirupam,Jana, Srabanti,Das, Aparoop
experimental part, p. 316 - 321 (2012/06/18)
With an objective to evaluate the antibacterial activity of triazine derivatives, a series of 2,4,6-trisubstituted-1,3,5-triazine were synthesized and characterized by FTIR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. The minimum inhibitory concentration (MIC) of the compounds that displayed favourable zone of inhibition was determined by broth microdilution method. Derivatives with morpholinyl substituent (4a and 4i) demonstrated good in vitro activities against Gram-positive organisms, whereas two of the compound bearing a diethylamino side chain exhibited moderate (4e) to broad spectrum (4j) activity comparable to streptomycin. The promising activity of the latter maybe attributed to the substitution of electron releasing group at para position of phenyl rings.
Synthesis and antibacterial evaluation of s-triazine based chalcones and their derivatives
Solankee, Anjani,Kapadia, Kishor,Solankee, Sejal,Patel, Ghanshyam
scheme or table, p. 837 - 840 (2010/06/15)
Various 2-(phenylamino/4′-substituted phenylamino)-4-(phenylainino/ 4′-substituted phenylamino)-6-[4′-{3″-(4?-{2′- (5′-ethylpyridin-2′-yl)-ethoxy}-phenyl)-2″-propenon-1″- yl}-phenylamino]-s-triazine 6(a-e) were prepared by reaction of different ketones 5(
Simple and efficient synthetic routes to bioactive s-triazinyl dithiocarbamate derivatives
Desai,Dodiya,Trivedi,Shah
, p. 495 - 506 (2008/12/23)
Series of 2,4-diarylamino-6-[N-(3′-methylphenyl)dithiocarbamoyl]-s- triazines (4a-l) and 2,4-bis[N-(3′-methylphenyl)dithiocarbamoyl]-6- arylamino-s-triazines (7a-l) were synthesized by two different synthetic routes. In the first route (A), 2,4,6-tricholoro-s-triazine (1) was condensed with N-(3-methylphenyl)ammoniumdithiocarbamate to afford compounds 3 or 6, which on reaction with different aryl amines afforded compounds 4a-l or 7a-l. In the second route (B), condensation of 1 with different aryl amines yielded compounds 2a-l or 5a-l. On further treatment with N-(3-methylphenyl) ammoniumdithiocarbamate these afforded compounds 4a-l or 7a-l. The newly synthesized compounds 4a-l and 7a-l were characterized by elemental analyses, infrared (IR), and 1H nuclear magnetic resonance (NMR) spectroscopic investigation. All the products were evaluated for their antibacterial and antifungal activity.
