4.6 Article

Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives

期刊

MOLECULES
卷 27, 期 7, 页码 -

出版社

MDPI
DOI: 10.3390/molecules27072061

关键词

diphenyl-1; 6-dihydropyrrolo [2; 3-b]pyrrole; hypocholesterolemic; hypotriglyceridemic activities; microwave irradiation; TC; TGs; LDL and ABTS method

资金

  1. Deanship of Scientific Research at Umm Al-Qura University [22UQU4331174DSR04]
  2. Taif University, Taif, Saudi Arabia [TURSP-2020/35]

向作者/读者索取更多资源

Novel pyrrolo [2,3-b] pyrrole derivatives with hypolipidemic and antimicrobial activities were synthesized and evaluated. Compounds 5 and 6 exhibited significant hypolipidemic effects, making them promising candidates for anti-atherosclerotic and hypolipidemic properties. Compound 2 showed moderate activity against Pseudomonas aeruginosa, while compound 3 demonstrated good antimicrobial activity against Staphylococcus aureus. These derivatives also displayed good anticancer activity against three tested cell lines.
Novel pyrrolo [2,3-b] pyrrole derivatives were synthesized and their hypolipidemic activity was assessed in hyperlipidemic rats. The chemical structures of the new derivatives were confirmed through spectral analysis. Compounds 5 and 6 were revealed to be the most effective hypolipidemic agents, with considerable hypocholesterolemic and hypotriglyceridemic effects. They appear to be promising candidates for creating new powerful derivatives with anti-atherosclerotic and hypolipidemic properties. As for antimicrobial activity, some of the tested compounds showed moderate activity against Pseudomonas aeruginosa: compound 2 revealed an MIC value of 50 mu g/mL, compared to 25 mu g/mL for ciprofloxacin. Compound 3 showed good antimicrobial activity against Staphylococcus aureus, comparable to ciprofloxacin, and roughly half the activity of ampicillin, according to MIC values. Compound 2 has an MIC approximately 25% of that of clotrimazole against Candida albicans. Compound 2 also showed the highest antioxidant activity with 59% inhibition of radical scavenging activity. Additionally, the cytotoxic activity of these new derivatives 1-7 was investigated and most of them showed good anticancer activity against the three tested cell lines.

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