Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives
The present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected ami...
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| Format: | Article |
| Language: | English |
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College of Pharmacy University of Baghdad
2017-03-01
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| Series: | Iraqi Journal of Pharmaceutical Sciences |
| Online Access: | https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/392 |
| _version_ | 1798024091803844608 |
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| author | Kasim S. Hmood Amer N. Elias |
| author_facet | Kasim S. Hmood Amer N. Elias |
| author_sort | Kasim S. Hmood |
| collection | DOAJ |
| description | The present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.
Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses have been carried out following simple methodology in excellent isolated yields.
The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR spectroscopy, and other physicochemical properties. All the final synthesized compounds were screened for their antimicrobial activity against selected microorganisms and showed excellent antibacterial and antifungal activities in comparison to Ceftriaxone, Cephalexin and Fluconazole.
The new Ceftriaxone derivatives have broadened the antimicrobial spectrum of the parent compound in having an extra antifungal activity in addition to its original antibacterial activity.
Keywords: Ceftriaxone, 2-aminothiazole, Antimicrobial activity, Antifungal activity, Ceftriaxone derivatives. |
| first_indexed | 2024-04-11T17:56:51Z |
| format | Article |
| id | doaj.art-c02f7ec0fc9444fc92246d99458750d1 |
| institution | Directory Open Access Journal |
| issn | 2521-3512 1683-3597 |
| language | English |
| last_indexed | 2024-04-11T17:56:51Z |
| publishDate | 2017-03-01 |
| publisher | College of Pharmacy University of Baghdad |
| record_format | Article |
| series | Iraqi Journal of Pharmaceutical Sciences |
| spelling | doaj.art-c02f7ec0fc9444fc92246d99458750d12022-12-22T04:10:45ZengCollege of Pharmacy University of BaghdadIraqi Journal of Pharmaceutical Sciences2521-35121683-35972017-03-0123210.31351/vol23iss2pp75-88Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone DerivativesKasim S. HmoodAmer N. EliasThe present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties. Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses have been carried out following simple methodology in excellent isolated yields. The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR spectroscopy, and other physicochemical properties. All the final synthesized compounds were screened for their antimicrobial activity against selected microorganisms and showed excellent antibacterial and antifungal activities in comparison to Ceftriaxone, Cephalexin and Fluconazole. The new Ceftriaxone derivatives have broadened the antimicrobial spectrum of the parent compound in having an extra antifungal activity in addition to its original antibacterial activity. Keywords: Ceftriaxone, 2-aminothiazole, Antimicrobial activity, Antifungal activity, Ceftriaxone derivatives.https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/392 |
| spellingShingle | Kasim S. Hmood Amer N. Elias Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives Iraqi Journal of Pharmaceutical Sciences |
| title | Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives |
| title_full | Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives |
| title_fullStr | Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives |
| title_full_unstemmed | Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives |
| title_short | Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives |
| title_sort | synthesis characterization and antimicrobial evaluation of new ceftriaxone derivatives |
| url | https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/392 |
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