104222-34-6Relevant articles and documents
Design and synthesis of benzothiazole schiff bases of potential antitumor activity
Al-Harthy, Thuraya,Abdel-Jalil, Raid,Zoghaib, Wajdi,Pflüger, Maren,Hofmann, Elisabeth,Hundsberger, Harald
, p. 1282 - 1292 (2016)
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.
Novel benzimidazole derivatives; synthesis, bioactivity and molecular docking study as potent urease inhibitors
Abdel-Jalil, Raid,Al-Sadi, Abdullah Mohammed,Amanlou, Massoud,Amini, Mohsen,Saeedian Moghadam, Ebrahim,Talebi, Meysam
, (2022/01/26)
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.]
Quinolonecarboxylic acid derivatives
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, (2008/06/13)
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
