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

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, wit...

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Autores principales: Kamel, Moumen S., Belal, Amany, Aboelez, Moustafa O., Shokr, E. Kh., Abdel-Ghany, H., Mansour, Hany S., Shawky, Ahmed M., El-Remaily, Mahmoud Abd El Aleem Ali Ali
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9000376/
https://www.ncbi.nlm.nih.gov/pubmed/35408463
http://dx.doi.org/10.3390/molecules27072061
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author Kamel, Moumen S.
Belal, Amany
Aboelez, Moustafa O.
Shokr, E. Kh.
Abdel-Ghany, H.
Mansour, Hany S.
Shawky, Ahmed M.
El-Remaily, Mahmoud Abd El Aleem Ali Ali
author_facet Kamel, Moumen S.
Belal, Amany
Aboelez, Moustafa O.
Shokr, E. Kh.
Abdel-Ghany, H.
Mansour, Hany S.
Shawky, Ahmed M.
El-Remaily, Mahmoud Abd El Aleem Ali Ali
author_sort Kamel, Moumen S.
collection PubMed
description 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.
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spelling pubmed-90003762022-04-12 Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives Kamel, Moumen S. Belal, Amany Aboelez, Moustafa O. Shokr, E. Kh. Abdel-Ghany, H. Mansour, Hany S. Shawky, Ahmed M. El-Remaily, Mahmoud Abd El Aleem Ali Ali Molecules Article 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. MDPI 2022-03-23 /pmc/articles/PMC9000376/ /pubmed/35408463 http://dx.doi.org/10.3390/molecules27072061 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Kamel, Moumen S.
Belal, Amany
Aboelez, Moustafa O.
Shokr, E. Kh.
Abdel-Ghany, H.
Mansour, Hany S.
Shawky, Ahmed M.
El-Remaily, Mahmoud Abd El Aleem Ali Ali
Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives
title Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives
title_full Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives
title_fullStr Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives
title_full_unstemmed Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives
title_short Microwave-Assisted Synthesis, Biological Activity Evaluation, Molecular Docking, and ADMET Studies of Some Novel Pyrrolo [2,3-b] Pyrrole Derivatives
title_sort microwave-assisted synthesis, biological activity evaluation, molecular docking, and admet studies of some novel pyrrolo [2,3-b] pyrrole derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9000376/
https://www.ncbi.nlm.nih.gov/pubmed/35408463
http://dx.doi.org/10.3390/molecules27072061
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