Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects
The common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant an...
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| Format: | Article |
| Language: | English |
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MDPI AG
2014-04-01
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| Series: | Antibiotics |
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| Online Access: | http://www.mdpi.com/2079-6382/3/2/128 |
| _version_ | 1818177877095481344 |
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| author | Monika I. Konaklieva |
| author_facet | Monika I. Konaklieva |
| author_sort | Monika I. Konaklieva |
| collection | DOAJ |
| description | The common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant antibiotics of such a magnitude that the conversation for antimicrobial drug development ought to include effective new antibiotics with alternative mechanisms of action. The electrophilic β-lactam ring is amenable for the inhibition of different enzyme classes by a suitable decoration of the core scaffold. Monocyclic β-lactams lacking an ionizable group at the lactam nitrogen exhibit target preferences toward bacterial enzymes important for resistance and virulence. The present review intends to draw attention to the versatility of the β-lactams as antimicrobials with “unusual” molecular targets. |
| first_indexed | 2024-12-11T20:39:04Z |
| format | Article |
| id | doaj.art-74ed88676bc142f3b99fdfbbef89e9ed |
| institution | Directory Open Access Journal |
| issn | 2079-6382 |
| language | English |
| last_indexed | 2024-12-11T20:39:04Z |
| publishDate | 2014-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antibiotics |
| spelling | doaj.art-74ed88676bc142f3b99fdfbbef89e9ed2022-12-22T00:51:34ZengMDPI AGAntibiotics2079-63822014-04-013212814210.3390/antibiotics3020128antibiotics3020128Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual SuspectsMonika I. Konaklieva0Department of Chemistry, American University, 4400 Massachusetts Ave. NW, Washington, DC, 20016-8014, USAThe common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant antibiotics of such a magnitude that the conversation for antimicrobial drug development ought to include effective new antibiotics with alternative mechanisms of action. The electrophilic β-lactam ring is amenable for the inhibition of different enzyme classes by a suitable decoration of the core scaffold. Monocyclic β-lactams lacking an ionizable group at the lactam nitrogen exhibit target preferences toward bacterial enzymes important for resistance and virulence. The present review intends to draw attention to the versatility of the β-lactams as antimicrobials with “unusual” molecular targets.http://www.mdpi.com/2079-6382/3/2/128antibiotic resistancedirected evolutionβ-lactams as chemical probes |
| spellingShingle | Monika I. Konaklieva Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects Antibiotics antibiotic resistance directed evolution β-lactams as chemical probes |
| title | Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects |
| title_full | Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects |
| title_fullStr | Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects |
| title_full_unstemmed | Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects |
| title_short | Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects |
| title_sort | molecular targets of β lactam based antimicrobials beyond the usual suspects |
| topic | antibiotic resistance directed evolution β-lactams as chemical probes |
| url | http://www.mdpi.com/2079-6382/3/2/128 |
| work_keys_str_mv | AT monikaikonaklieva moleculartargetsofblactambasedantimicrobialsbeyondtheusualsuspects |