877-90-7Relevant articles and documents
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.]
A Different Approach to the EGFR Inhibitor Gefitinib Involving Solid-Phase Synthesis
Sequeira, André,Louren?o, Ana,Ferreira, Luísa Maria,Branco, Paula Sério,Mendes, Zita,Louren?o, Nuno M. T.,Figueiredo, Margarida,Carvalho, Luísa C. R.
, p. 1346 - 1350 (2018/05/16)
An efficient solid-phase synthesis approach is here reported for the first time to prepare the EGFR inhibitor Gefitinib. The five-step synthetic strategy used FMP resin as the solid support, and FTIR and colorimetric assays were used to track the reaction's progress. Gefitinib was obtained with an overall yield of 40%.
Synthesis and antimalarial activity of Baylis-Hillman adducts from substituted 2-chloroquinoline-3-carboxaldehydes
Srihari, Ejjirothu,Kumar, Gangala Siva,Kumar, Chebolu Naga Sesha Sai Pavan,Seth, Ratnesh Kumar,Biswas, Sukla,Sridhar, Balasubramanian,Rao, Vaidya Jayathirtha
scheme or table, p. 111 - 119 (2011/11/30)
Various quinoline carboxaldehydes were prepared from corresponding anilides using classical Vilsmeier-Haack reaction conditions and transformed into their Baylis-Hillman adducts. The synthesized Baylis-Hillman adducts were screened for their in vitro antimalarial activity against Plasmodium falciparum . Most of the compounds out of 21 compounds synthesized and screened exhibited substantial antimalarial activity. by Walter de Gruyter.