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

Authors :
Moumen S. Kamel
Amany Belal
Moustafa O. Aboelez
E. Kh. Shokr
H. Abdel-Ghany
Hany S. Mansour
Ahmed M. Shawky
Mahmoud Abd El Aleem Ali Ali El-Remaily
Source :
Molecules, Vol 27, Iss 7, p 2061 (2022)
Publication Year :
2022
Publisher :
MDPI AG, 2022.

Abstract

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 μg/mL, compared to 25 μg/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.

Details

Language :
English
ISSN :
27072061 and 14203049
Volume :
27
Issue :
7
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.181866d52c964b70b9e470ed556d90e2
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules27072061