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Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment
A new chemical library based on the hybridization of cholic acid with the heterocyclic moiety 1,3,4-oxadizole was synthesized, and tested for antimicrobial activity against Gram-positive, Gram-negative bacteria, and fungi. Among the synthesized compounds, the most potent derivatives against S. aureu...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Beilstein-Institut
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9174839/ https://www.ncbi.nlm.nih.gov/pubmed/35706993 http://dx.doi.org/10.3762/bjoc.18.63 |
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author | Rasras, Anas J El-Naggar, Mohamed Safwat, Nesreen A Al-Qawasmeh, Raed A |
author_facet | Rasras, Anas J El-Naggar, Mohamed Safwat, Nesreen A Al-Qawasmeh, Raed A |
author_sort | Rasras, Anas J |
collection | PubMed |
description | A new chemical library based on the hybridization of cholic acid with the heterocyclic moiety 1,3,4-oxadizole was synthesized, and tested for antimicrobial activity against Gram-positive, Gram-negative bacteria, and fungi. Among the synthesized compounds, the most potent derivatives against S. aureus were 4t, 4i, 4p, and 4c with MIC values between 31 and 70 µg/mL, while compound 4p was the most active one against Bacillus subtilis with a MIC value of 70 µg/mL. Interestingly, compounds 4a and 4u exerted selective activity against Gram-positive bacteria. The synthesized compounds showed good activity against A. fumigatus and C. albicans and compound 4v exhibited selective activity against fungi only. |
format | Online Article Text |
id | pubmed-9174839 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Beilstein-Institut |
record_format | MEDLINE/PubMed |
spelling | pubmed-91748392022-06-14 Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment Rasras, Anas J El-Naggar, Mohamed Safwat, Nesreen A Al-Qawasmeh, Raed A Beilstein J Org Chem Full Research Paper A new chemical library based on the hybridization of cholic acid with the heterocyclic moiety 1,3,4-oxadizole was synthesized, and tested for antimicrobial activity against Gram-positive, Gram-negative bacteria, and fungi. Among the synthesized compounds, the most potent derivatives against S. aureus were 4t, 4i, 4p, and 4c with MIC values between 31 and 70 µg/mL, while compound 4p was the most active one against Bacillus subtilis with a MIC value of 70 µg/mL. Interestingly, compounds 4a and 4u exerted selective activity against Gram-positive bacteria. The synthesized compounds showed good activity against A. fumigatus and C. albicans and compound 4v exhibited selective activity against fungi only. Beilstein-Institut 2022-05-31 /pmc/articles/PMC9174839/ /pubmed/35706993 http://dx.doi.org/10.3762/bjoc.18.63 Text en Copyright © 2022, Rasras et al. https://creativecommons.org/licenses/by/4.0/This is an open access article licensed under the terms of the Beilstein-Institut Open Access License Agreement (https://www.beilstein-journals.org/bjoc/terms/terms), which is identical to the Creative Commons Attribution 4.0 International License (https://creativecommons.org/licenses/by/4.0 (https://creativecommons.org/licenses/by/4.0/) ). The reuse of material under this license requires that the author(s), source and license are credited. Third-party material in this article could be subject to other licenses (typically indicated in the credit line), and in this case, users are required to obtain permission from the license holder to reuse the material. |
spellingShingle | Full Research Paper Rasras, Anas J El-Naggar, Mohamed Safwat, Nesreen A Al-Qawasmeh, Raed A Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment |
title | Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment |
title_full | Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment |
title_fullStr | Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment |
title_full_unstemmed | Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment |
title_short | Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment |
title_sort | cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment |
topic | Full Research Paper |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9174839/ https://www.ncbi.nlm.nih.gov/pubmed/35706993 http://dx.doi.org/10.3762/bjoc.18.63 |
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