81962-58-5Relevant academic research and scientific papers
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.]
Design, synthesis and anti-HIV activity of novel quinoxaline derivatives
Patel, Saloni B.,Patel, Bhumika D.,Pannecouque, Christophe,Bhatt, Hardik G.
, p. 230 - 240 (2016/04/26)
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
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 (2016/07/26)
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.
6-FLUORO-7-(1-PIPERAZINYL)QUINOXALINE 1,4-DIOXIDES. PART I. 2-(N-2-HYDROXYALKYLCARBAMOYL) DERIVATIVES
El-Abadelah, Mustafa M.,Nazer, Musa Z.,El-Abadla, Naser S.,Meier, Herbert
, p. 2203 - 2220 (2007/10/03)
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.
Quinolonecarboxylic acid derivatives
-
, (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
Pyrroloquinoline and benzoquinolizine compounds and antimicrobial compositions
-
, (2008/06/13)
A benzoheterocyclic compound of the formula (I) STR1 wherein R1, R2, R3 and n are as defined, and its pharmaceutically acceptable salts, processes for preparing same and antibacterial composition containing the benzoheterocyclic compound as an active ingredient and a pharmaceutically acceptable carrier are disclosed.
