A novel benzothiazole-1,2,3-triazole-based arene osmium(II) complex as an effective rhabdomyosarcoma cancer stem cell agent
Sofia SharkawyAlba Hernández-GarcíaHana KostrhunováDelia BautistaLenka MarkováM. Dolores SantanaJana KašpárkováViktor BrabecJosé Ruiz
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We designed a series of pseudo-octahedral arene Os(II) complexes ( Os1 – Os5 ) with the general formula [(η 6 - p -cym)Os(BTAT)Cl] + , where BTAT represents chelating N^N′ ligands based on the 1-aryl-4-benzothiazolyl-1,2,3-triazole scaffold. The structures of Os3 ...Keywords:
Benzothiazole
Osmium
Triazole
A series of novel fluorinated heterocyclic hybrid molecules based on triazole & quinoxaline scaffold were designed, synthesized and evaluated for inhibition of Plasmodium falciparum, a virulent human malaria parasite. Mono and bis triazole tagged quinoxaline analogs were synthesized by propargylation of 6-amino quinoxaline followed by click reaction with various substituted aromatic azides under uncertain reaction conditions. The newly synthesized molecules were assessed for antimalarial activity and three of the analogs were identified as promising leads which killed parasites with IC50 values <10 μM and showed 27-70 selective indices. Keywords: Antimalarials, click reaction, hybrid molecules, plasmodium, quinoxalines, triazoles.
Quinoxaline
Triazole
Lead compound
1,2,3-Triazole
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Copper(I)-catalyzed azide alkyne cycloaddition (CuAAC) methodology to develop a library of 3-methyl quinoxaline-1,2,3-triazole hybrid molecules. The designed molecules were synthesized via efficient and purification free method. The structures of the achieved compounds were recognized based on their spectral data. The antimicrobial activity for the synthesized compounds was evaluated against four bacterial species and two fungal strains. Six compounds are broad spectrum molecule, which can inhibit the growth of both Gram-positive and Gram-negative bacteria. Two molecules show mainly antifungal activity. Compound 6e shows highest antibacterial as well as antifungal activity.
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Triazole
Alkyne
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New four-component benzoxazole and benzothiazole scaffolds were obtained via an Ugi-Smiles coupling of 2-mercapto benzoxazole and 2-mercapto benzothiazole derivatives with isocyanides, aldehydes and primary amines. The 2-mercapto benzimidazoles tested were not reactive under similar conditions as well as the analogous 2-hydroxy benzoxazoles and 2-hydroxy benzothiazoles.
Benzothiazole
Benzoxazole
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In the title compound, C14H9N3S, the triazole and benzothiazole moieties are coplanar. The dihedral angle between the fused triazole–benzothiazole fragment and the phenyl ring is 39.20 (5)°. The structure is stabilized by C—H⋯N intermolecular interactions.
Benzothiazole
Dihedral angle
Triazole
1,2,4-Triazole
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One-pot protocol for the synthesis of novel class of triazole linked 2-sugar and 2-aryl substituted benzimidazoles has been developed. The rapid and simple method involves copper (I) catalyzed simultaneous formation of benzimidazole and triazole rings at room temperature and in high yield.
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Triazole
One-pot synthesis
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Benzothiazole
Amperometry
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A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3-triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. Three different linkers were used to optimise the enzyme inhibitory effect. Out of the 20 compounds, 13 showed some AChE inhibition. The most potent compound, which showed 84% inhibition at 100 μM, contained a 1-(2-fluorobenzyl)-1,2,3-triazole linked to a benzimidazole group. A docking simulation study showed that the most active compound bound preferentially to the catalytic anionic subsite of the AChE enzyme.
Benzothiazole
Benzimidazole
Triazole
1,2,4-Triazole
Docking (animal)
1,2,3-Triazole
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Background: The synthesis of triazole derivatives is a major interest among synthetic organic chemists. Indeed, triazole derivatives, especially containing fluorine atom, present wide applications in the field of science materials. In this aim, we have developed this work to propose a new route for the synthesis of fluorinated triazole derivatives. Methods: Various acetylenic compounds derived from γ- and δ-lactam on reaction with using γ- and δ-lactam and sodium azide in the presence of 5 mol% of copper nanoparticles in water to offered triazole derivatives. Results: Replacement of CH3CN with H2O as a solvent, for the reaction catalyzed by CuNPs to produce fluorinated triazole, was finished within 1 h in 90% yield. Conclusion: A simple and efficient protocol for the synthesis of 1,2,3-triazole derivatives using 5 % of copper nanoparticles was developed. Keywords: Azido-fluoro-D-glucopyranose, click glycosylation, fluoro 1, 2, 3-triazole.
Triazole
Sodium azide
1,2,3-Triazole
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2-hydrazino-benzothiazole was synthesized by the benzothiazole and hydrazine hydrate and 6-bromo-2-hydrazino-benzothiazole was synthesized by brom(o)-. 0-[(6 bromo-2-benzothiazole hydrazono) methyl] phenol was also synthesized by 6-bromo-2-hydrazino-benzothiazole and salicylide .the different modified benzothiazole also was synthesized . The effects of mould proofing of different benzothiazole derivate to leather were investigated. The results shows there are good effects that benzothiazole derivate to leather . that the effect of mildewproof was better by brom (o)-and form of Schiff's base .this show there is effective of structure stratum of activity by brom(o)-and form of Schiff's base .
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Hydrazine (antidepressant)
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To develop potent anticancer compounds using benzothiazole scaffolds GQSAR analysis was performed on 41 reported benzothiazole derivatives for identification of structural fragments. Benzothiazole dataset was fragmented in to two fragments (R1 and R2). GQSAR models were generated using MLR. GQSAR analysis revealed presence of hydrophobic groups on R1 will potentiate anticancer activity. The generated models are giving insight into the benzothiazole structural requirements which will be optimized for design of anticancer drugs. :TJPS-2019-0123.R1
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