Nα ‐Aroyl‐ N ‐Aryl‐Phenylalanine Amides: A Promising Class of Antimycobacterial Agents Targeting the RNA Polymerase
Abstract: Tuberculosis (TB), caused by Mycobacterium tuberculosis, remains the leading cause of death from a bacterium in the world. The global prevalence of clinically relevant infections with opportunistically pathogenic non‐tuberculous mycobacteria (NTM) has also been on the rise. Pharmacological treatment of both TB and NTM infections usually requires prolonged regimens of drug combinations, and is often challenging because of developed or inherent resistance to common antibiotic drugs. Medicinal chemistry efforts are thus needed to improve treatment options and therapeutic outcomes. Nα‐aroyl‐N‐aryl‐phenylalanine amides (AAPs) have been identified as potent antimycobacterial agents that target the RNA polymerase with a low probability of cross resistance to rifamycins, the clinically most important class of antibiotics known to inhibit the bacterial RNA polymerase. In this review, we describe recent developments in the field of AAPs, including synthesis, structural characterization, in vitro microbiological profiling, structure‐activity relationships, physicochemical properties, pharmacokinetics and early cytotoxicity assessment.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Nα ‐Aroyl‐ N ‐Aryl‐Phenylalanine Amides: A Promising Class of Antimycobacterial Agents Targeting the RNA Polymerase ; day:08 ; month:05 ; year:2024 ; extent:15
Chemistry & biodiversity ; (08.05.2024) (gesamt 15)
- Creator
- DOI
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10.1002/cbdv.202400267
- URN
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urn:nbn:de:101:1-2405091410588.730030365769
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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14.08.2025, 10:56 AM CEST
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Seidel, Rüdiger W.
- Goddard, Richard
- Lang, Markus
- Richter, Adrian
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Mechanochemical Synthesis of N‐Aryl Amides from O‐Protected Hydroxamic Acids
Photo‐Induced Carbonylation of Aryl Bromides for the Synthesis of Aryl Esters and Amides Under Transition Metal‐Free Conditions
Multiple implications of an active site phenylalanine in the catalysis of aryl-alcohol oxidase
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Synthesis and characterization of Nα-aroyl-N-aryl-phenylalanine amides and their activity against mycobacteria
Synthesis and in vitro Metabolic Stability of Sterically Shielded Antimycobacterial Phenylalanine Amides
Mechanochemical Synthesis of N‐Aryl Amides from O‐Protected Hydroxamic Acids
Photo‐Induced Carbonylation of Aryl Bromides for the Synthesis of Aryl Esters and Amides Under Transition Metal‐Free Conditions
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