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Nα-Aroyl-N-Aryl-Phenylalanine Amides: A Promising Class of Antimycobacterial Agents Targeting the RNA Polymerase.
- Source :
-
Chemistry & biodiversity [Chem Biodivers] 2024 Jun; Vol. 21 (6), pp. e202400267. Date of Electronic Publication: 2024 May 08. - Publication Year :
- 2024
-
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.<br /> (© 2024 The Authors. Chemistry & Biodiversity published by Wiley-VHCA AG.)
- Subjects :
- Humans
Microbial Sensitivity Tests
Mycobacterium tuberculosis drug effects
Mycobacterium tuberculosis enzymology
Structure-Activity Relationship
Antitubercular Agents pharmacology
Antitubercular Agents chemistry
Antitubercular Agents chemical synthesis
Molecular Structure
Anti-Bacterial Agents pharmacology
Anti-Bacterial Agents chemistry
Anti-Bacterial Agents chemical synthesis
Amides chemistry
Amides pharmacology
Amides chemical synthesis
DNA-Directed RNA Polymerases antagonists & inhibitors
DNA-Directed RNA Polymerases metabolism
Phenylalanine pharmacology
Phenylalanine chemistry
Phenylalanine chemical synthesis
Phenylalanine analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 1612-1880
- Volume :
- 21
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Chemistry & biodiversity
- Publication Type :
- Academic Journal
- Accession number :
- 38588490
- Full Text :
- https://doi.org/10.1002/cbdv.202400267