Lea Mann
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View article: Design, Synthesis, and Biological Evaluation of Mono- and Diamino-Substituted Squaramide Derivatives as Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthase
Design, Synthesis, and Biological Evaluation of Mono- and Diamino-Substituted Squaramide Derivatives as Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthase Open
Amides of squaric acid are new drug candidates with activity against mycobacteria. Like the approved drug bedaquiline, these compounds achieve efficacy by inhibiting mycobacterial ATP synthase. However, squaramides have a different binding…
View article: Next-generation rifamycins for the treatment of mycobacterial infections
Next-generation rifamycins for the treatment of mycobacterial infections Open
Mycobacterium abscessus is a rapidly growing nontuberculous Mycobacterium causing severe pulmonary infections, especially in immunocompromised individuals and patients with underlying lung conditions like cystic fibrosis (CF). While rifamy…
View article: Synthesis and Antimycobacterial Assays of Some New Ethambutol Analogs
Synthesis and Antimycobacterial Assays of Some New Ethambutol Analogs Open
Ethambutol (EMB) is a first-line anti-tuberculosis drug that is also considered in treatment regimens for infections caused by non-tuberculous mycobacteria (NTM). EMB targets the arabinosyl transferases EmbCAB, which are important for the …
View article: Determination of bactericidal activity against 3HC-2-Tre-labelled Mycobacterium abscessus (Mycobacteroides abscessus) by automated fluorescence microscopy
Determination of bactericidal activity against 3HC-2-Tre-labelled Mycobacterium abscessus (Mycobacteroides abscessus) by automated fluorescence microscopy Open
The minimum bactericidal concentration (MBC) of antibiotics is an important parameter for the potency of a drug in eradicating a bacterium as well as an important measure of the potential of a drug candidate in research and development. We…
View article: Synthesis and <i>in vitro</i> Metabolic Stability of Sterically Shielded Antimycobacterial Phenylalanine Amides
Synthesis and <i>in vitro</i> Metabolic Stability of Sterically Shielded Antimycobacterial Phenylalanine Amides Open
N α‐aroyl‐ N ‐aryl‐phenylalanine amides (AAPs) are RNA polymerase inhibitors with activity against Mycobacterium tuberculosis and non‐tuberculous mycobacteria. We observed that AAPs rapidly degrade in microsomal suspensions, suggesting tha…
View article: Structural characterization of a 3-hydroxychromone dye trehalose conjugate for fluorescent labelling of mycobacteria
Structural characterization of a 3-hydroxychromone dye trehalose conjugate for fluorescent labelling of mycobacteria Open
3-Hydroxychromone (3HC) dye trehalose conjugates have previously been exploited as environment-sensitive fluorescent labels to detect mycobacteria by fluorescence microscopy. We have studied the 3HC dye 2-(6-(diethylamino)benzofuran-2-yl)-…
View article: CCDC 2258616: Experimental Crystal Structure Determination
CCDC 2258616: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Imidazopyridine Amides: Synthesis, <i>Mycobacterium smegmatis</i> CIII<sub>2</sub>CIV<sub>2</sub> Supercomplex Binding, and In Vitro Antimycobacterial Activity
Imidazopyridine Amides: Synthesis, <i>Mycobacterium smegmatis</i> CIII<sub>2</sub>CIV<sub>2</sub> Supercomplex Binding, and In Vitro Antimycobacterial Activity Open
Q203 (telacebec) is an imidazopyridine amide (IPA) targeting the respiratory CIII2CIV2 supercomplex of the mycobacterial electron transport chain (ETC). Aiming for a better understanding of the molecular mechanism of action of IPA, 27 anal…
View article: Structural Elucidation of 2-(6-(Diethylamino)benzofuran-2-yl)-3-hydroxy-4H-chromen-4-one and Labelling of Mycobacterium aurum Cells
Structural Elucidation of 2-(6-(Diethylamino)benzofuran-2-yl)-3-hydroxy-4H-chromen-4-one and Labelling of Mycobacterium aurum Cells Open
Trehalose conjugates of 3-hydroxychromone (3HC) dyes have previously been utilized as fluorescence labels to detect metabolically active mycobacteria with a view to facilitating point-of-care detection of mycobacterial pathogens, especiall…
View article: CCDC 2231847: Experimental Crystal Structure Determination
CCDC 2231847: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2231845: Experimental Crystal Structure Determination
CCDC 2231845: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2231846: Experimental Crystal Structure Determination
CCDC 2231846: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Synthesis and Characterization of Phenylalanine Amides Active against <i>Mycobacterium abscessus</i> and Other Mycobacteria
Synthesis and Characterization of Phenylalanine Amides Active against <i>Mycobacterium abscessus</i> and Other Mycobacteria Open
Nα-2-thiophenoyl-d-phenylalanine-2-morpholinoanilide [MMV688845, Pathogen Box; Medicines for Malaria Venture; IUPAC: (2R)-N-(1-((2-morpholinophenyl)amino)-1-oxo-3-phenylpropan-2-yl)thiophene-2-carboxamide)] is a hit compound, which shows a…
View article: Structural basis for inhibition of mycobacterial ATP synthase by squaramides and second generation diarylquinolines
Structural basis for inhibition of mycobacterial ATP synthase by squaramides and second generation diarylquinolines Open
Mycobacteria, such as Mycobacterium tuberculosis , depend on the activity of adenosine triphosphate (ATP) synthase for growth. The diarylquinoline bedaquiline (BDQ), a mycobacterial ATP synthase inhibitor, is an important medication for tr…
View article: <i>In Vitro</i> Profiling of the Synthetic RNA Polymerase Inhibitor MMV688845 against Mycobacterium abscessus
<i>In Vitro</i> Profiling of the Synthetic RNA Polymerase Inhibitor MMV688845 against Mycobacterium abscessus Open
Infections with nontuberculous mycobacteria are an increasing health problem, and only a few new drug classes show activity against these multidrug-resistant bacteria. Due to insufficient therapy options, the development of new drug leads …
View article: CCDC 2171380: Experimental Crystal Structure Determination
CCDC 2171380: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2171377: Experimental Crystal Structure Determination
CCDC 2171377: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: BTZ-Derived Benzisothiazolinones with In Vitro Activity against <i>Mycobacterium tuberculosis</i>
BTZ-Derived Benzisothiazolinones with In Vitro Activity against <i>Mycobacterium tuberculosis</i> Open
[Image: see text] 8-Nitro-1,3-benzothiazin-4-ones (BTZs) are known as potent antitubercular agents. BTZ043 as one of the most advanced compounds has reached clinical trials. The putative oxidation products of BTZ043, namely, the correspond…
View article: CCDC 2171378: Experimental Crystal Structure Determination
CCDC 2171378: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2171379: Experimental Crystal Structure Determination
CCDC 2171379: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Structure–Activity Relationship of Anti-<i>Mycobacterium abscessus</i> Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors
Structure–Activity Relationship of Anti-<i>Mycobacterium abscessus</i> Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors Open
Mycobacterium abscessus causes difficult-to-cure pulmonary infections. The bacterium is resistant to most anti-infective agents, including first line antituberculosis (anti-TB) drugs. MMV688844 (844) is a piperidine-4-carboxamide (P4C) wit…
View article: CCDC 2049487: Experimental Crystal Structure Determination
CCDC 2049487: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: In Vivo Antimalarial Activity of Leaf Extracts and a Major Compound Isolated from Ranunculus multifidus Forsk
In Vivo Antimalarial Activity of Leaf Extracts and a Major Compound Isolated from Ranunculus multifidus Forsk Open
The leaves of Ranunculus multifidus Forsk. are traditionally used for the treatment of malaria in several African countries. In the present study, 80% methanol (RM-M) and hydrodistilled (RM-H) extracts of fresh leaves from R. multifidus an…