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- Pham, Em Canh, et al.
(författare)
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N,2,6-Trisubstituted 1H-benzimidazole derivatives as a new scaffold of antimicrobial and anticancer agents : design, synthesis, in vitro evaluation, and in silico studies
- 2023
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Ingår i: RSC Advances. - : Royal Society of Chemistry. - 2046-2069. ; 13:1, s. 399-420
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Tidskriftsartikel (refereegranskat)abstract
- Compounds containing benzimidazole moiety occupy privileged chemical space for discovering new bioactive substances. In continuation of our recent work, 69 benzimidazole derivatives were designed and synthesized with good to excellent yields of 46-99% using efficient synthesis protocol i.e. sodium metabisulfite catalyzed condensation of aromatic aldehydes with o-phenylenediamines to form 2-arylbenzimidazole derivatives followed by N-alkylation by conventional heating or microwave irradiation for diversification. Potent antibacterial compounds against MSSA and MRSA were discovered such as benzimidazole compounds 3k (2-(4-nitrophenyl), N-benzyl), 3l (2-(4-chlorophenyl), N-(4-chlorobenzyl)), 4c (2-(4-chlorophenyl), 6-methyl, N-benzyl), 4g (2-(4-nitrophenyl), 6-methyl, N-benzyl), and 4j (2-(4-nitrophenyl), 6-methyl, N-(4-chlorobenzyl)) with MIC of 4-16 mu g mL(-1). In addition, compound 4c showed good antimicrobial activities (MIC = 16 mu g mL(-1)) against the bacteria strains Escherichia coli and Streptococcus faecalis. Moreover, compounds 3k, 3l, 4c, 4g, and 4j have been found to kill HepG2, MDA-MB-231, MCF7, RMS, and C26 cancer cells with low mu M IC50 (2.39-10.95). These compounds showed comparable drug-like properties as ciprofloxacin, fluconazole, and paclitaxel in computational ADMET profiling. Finally, docking studies were used to assess potential protein targets responsible for their biological activities. Especially, we found that DHFR is a promising target both in silico and in vitro with compound 4c having IC50 of 2.35 mu M.
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| 2. |
- Yatan Pal Singh, Balhara, et al.
(författare)
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Can daily internet use time screen for problematic internet use among college students? A receiver operator characteristic curve-based multi-country study
- 2020
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Ingår i: Neurology Psychiatry and Brain Research. - : Elsevier BV. - 0941-9500 .- 2212-8581. ; 38, s. 43-48
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Tidskriftsartikel (refereegranskat)abstract
- © 2020 Elsevier GmbH Background and objective: The current article explored the possibility of using daily internet use time as an indicator for problematic internet use (PIU) among college/ university students based on observations from a multi-centric, multi-country study conducted across eight different countries. Additionally, the current article explored whether daily night time sleep and physical activity can serve as possible indicators of PIU. Methods: The present article presents the findings from analysis of information collected from 2643 college/university students from eight countries. Area under the ROC curve (AUC) was calculated to compare the predictive performance of three different indicator variables in the study participants to determine PIU. Results: The AUC for daily internet use time was 0.64 (95 % CI: 0.62 to 0.656), which was higher than the AUC for weekly physical activity (0.599; 95 % CI: 0.580 to 0.618) and daily night time sleep (0.563; 95 % CI: 0.544 to 0.582). The AUC for three indicator variables was compared, which showed that the AUC for daily internet time was significantly higher than the AUC for daily night-time sleep. Conclusions: The assessment of daily internet use time as part of a larger battery of general health-related questions could be applied periodically among young students for screening of PIU in addition to a host of other important mental and physical health related conditions and behaviors. However, further studies are needed to determine optimal cut-off depending upon the desired trade-off between sensitivity and specificity for screening among different populations.
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