- Design and synthesis of benzothiazole schiff bases of potential antitumor activity
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In an attempt to develop a new class of selective antitumor agents, a novel series of benzothiazole derivatives was prepared via the condensation of 5-fluoro-6-(4-methylpiperazin-1-yl)benzo[d]thiazol-2- Amine with aromatic aldehydes. The preliminary bioassay reveals that (4-fluorobenzylidene)-[5-fluoro-6-(4-methylpiperazin-1-yl)-benzothiazol-2-yl]- Amine show specific anticancer cytotoxicity.
- Al-Harthy, Thuraya,Abdel-Jalil, Raid,Zoghaib, Wajdi,Pflüger, Maren,Hofmann, Elisabeth,Hundsberger, Harald
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- Design, synthesis and anti-HIV activity of novel quinoxaline derivatives
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In order to design novel anti-HIV agents, pharmacophore modelling, virtual screening, 3D-QSAR and molecular docking studies were performed. Pharmacophore model was generated using 17 structurally diverse molecules using DISCOtech followed by refinement wi
- Patel, Saloni B.,Patel, Bhumika D.,Pannecouque, Christophe,Bhatt, Hardik G.
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- Novel benzimidazole derivatives; synthesis, bioactivity and molecular docking study as potent urease inhibitors
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Background: Benzimidazole derivatives?are?widely?used?to?design and?synthesize?novel bioactive compounds.?There are several approved benzimidazole-based?drugs?on?the?market. Objectives: In this study, we aimed to design and?synthesize?a series of novel benzimidazole derivatives 8a-n?that?are?urease inhibitors. Methods: All 8a-n were synthesized in a multistep. To determine the urease inhibitory effect of 8a-n, the urease inhibition kit was used. The cytotoxicity assay of 8a-n was determined using MTT method. Molecular modelling was determined using autodock software. Results: All?8a-n were synthesized in high yield, and their structures were determined using 1H-NMR, 13C-NMR, MS, and elemental analyses. In compared to thiourea and hydroxyurea as standards (IC50: 22 and 100?μM, respectively), all 8a-n had stronger urease inhibition activity (IC50: 3.36—10.81?μM). With an IC50 value of 3.36?μM, 8e had the best enzyme inhibitory activity. On two evaluated cell lines, the MTT cytotoxicity experiment revealed that all 8a-n have IC50 values greater than 50?μM. Finally, a docking investigation revealed a plausible way of interaction between the 8e and 8d and the enzyme's active site's key residues. Conclusion: The synthesized benzimidazole derivatives exhibit high activity, suggesting that further research on this family of compounds would be beneficial to finding a potent urease inhibitor. Graphical abstract: [Figure not available: see fulltext.]
- Abdel-Jalil, Raid,Al-Sadi, Abdullah Mohammed,Amanlou, Massoud,Amini, Mohsen,Saeedian Moghadam, Ebrahim,Talebi, Meysam
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- 6-FLUORO-7-(1-PIPERAZINYL)QUINOXALINE 1,4-DIOXIDES. PART I. 2-(N-2-HYDROXYALKYLCARBAMOYL) DERIVATIVES
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A series of N--β-aminoalkanol 1,4-dioxides (12a-h) have been synthesized for bioassay via the Beirut reaction of 5(6)-fluoro-6(5)-(4-methyl-1-piperazinyl)benzofuroxan (9) with the appropriate N-acetoacetyl-β-aminoalkanol in the presence of triethylamine.Preliminary in vitro investigations have indicated that none of the title compounds exhibits any significant antibacterial potency at concentrations /= 200 μg/ml.
- El-Abadelah, Mustafa M.,Nazer, Musa Z.,El-Abadla, Naser S.,Meier, Herbert
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p. 2203 - 2220
(2007/10/03)
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- Quinolonecarboxylic acid derivatives
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Quinolonecarboxylic acid derivatives of the following formula, STR1 wherein R1, R2, R3 and R4 are each independently hydrogen atom or lower alkyl group; the hydrates or the pharmaceutically acceptable acid addit
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