scholarly journals Biological evaluation of a novel nitroimidazooxazole derivative, IIIM-MCD-019 against Mycobacterium tuberculosis and its in vivo efficacy

2016 ◽  
Vol 45 ◽  
pp. 414
Author(s):  
S. Singh ◽  
G. Munagala ◽  
K.Y. Reddy ◽  
S.K. Bhola ◽  
R. Chib ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Biological Evaluation ◽  
In Vivo Efficacy

scholarly journals Intracellular localisation of Mycobacterium tuberculosis affects efficacy of the antibiotic pyrazinamide

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Pierre Santucci ◽  
Daniel J. Greenwood ◽  
Antony Fearns ◽  
Kai Chen ◽  
Haibo Jiang ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Host Cell ◽  
Combination Chemotherapy ◽  
In Vitro Activity ◽  
In Vivo Efficacy ◽  
Human Macrophages ◽  
Ion Microscopy ◽  
Intracellular Localisation

AbstractTo be effective, chemotherapy against tuberculosis (TB) must kill the intracellular population of the pathogen, Mycobacterium tuberculosis. However, how host cell microenvironments affect antibiotic accumulation and efficacy remains unclear. Here, we use correlative light, electron, and ion microscopy to investigate how various microenvironments within human macrophages affect the activity of pyrazinamide (PZA), a key antibiotic against TB. We show that PZA accumulates heterogeneously among individual bacteria in multiple host cell environments. Crucially, PZA accumulation and efficacy is maximal within acidified phagosomes. Bedaquiline, another antibiotic commonly used in combined TB therapy, enhances PZA accumulation via a host cell-mediated mechanism. Thus, intracellular localisation and specific microenvironments affect PZA accumulation and efficacy. Our results may explain the potent in vivo efficacy of PZA, compared to its modest in vitro activity, and its critical contribution to TB combination chemotherapy.

Synthesis and biological evaluation of mixed-ligands cyclometalated iridium(III)-quinoline complexes

2021 ◽  
Author(s):  
Yan Yang ◽  
Cheng-Ming Wang ◽  
Feng-Hua Pan ◽  
Qi-Pin Qin ◽  
Qiu-Ji Xie ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
In Vivo Efficacy ◽  
Mixed Ligands ◽  
Synthesis And Biological Evaluation ◽  
Insight Into

With the aim of gaining new insight into the underlying apoptosis mechanisms and in vivo efficacy of cyclometalated Ir(III) complexes as metalodrugs, six new cyclometalated Ir(III)-quinoline complexes, [Ir(1a)(2pq)2] (2a), [Ir(1b)(2pq)2]...

scholarly journals Evaluation of a 2-Pyridone, KRQ-10018, against Mycobacterium tuberculosis In Vitro and In Vivo

2008 ◽  
Vol 52 (4) ◽  
pp. 1513-1515 ◽  
Author(s):  
Anne J. Lenaerts ◽  
Casey Bitting ◽  
Lisa Woolhiser ◽  
Veronica Gruppo ◽  
Karen S. Marietta ◽  
...  
Keyword(s):  
Body Weight ◽  
Mycobacterium Tuberculosis ◽  
In Vivo Efficacy

ABSTRACT A novel subclass of quinolones, 2-pyridones, showed potent activity against Mycobacterium tuberculosis, with KRQ-10018 being an early lead. KRQ-10018 showed better activity in vitro against M. tuberculosis versus moxifloxacin. In vivo efficacy of KRQ-10018 at 300 mg/kg of body weight was similar to that of isoniazid at 25 mg/kg, but showed less activity than moxifloxacin at 300 mg/kg.

Synthesis and Biological Evaluation ofN,N′-Squaramides with High in Vivo Efficacy and Low Toxicity: Toward a Low-Cost Drug against Chagas Disease

2014 ◽  
Vol 57 (3) ◽  
pp. 987-999 ◽  
Author(s):  
Francisco Olmo ◽  
Carmen Rotger ◽  
Inmaculada Ramírez-Macías ◽  
Luis Martínez ◽  
Clotilde Marín ◽  
...  
Keyword(s):  
Chagas Disease ◽  
Low Cost ◽  
Biological Evaluation ◽  
In Vivo Efficacy ◽  
Low Toxicity ◽  
Synthesis And Biological Evaluation

scholarly journals Pentacyclic Nitrofurans with In Vivo Efficacy and Activity against Nonreplicating Mycobacterium tuberculosis

PLoS ONE ◽  
2014 ◽  
Vol 9 (2) ◽  
pp. e87909 ◽  
Author(s):  
Rakesh ◽  
David F. Bruhn ◽  
Michael S. Scherman ◽  
Lisa K. Woolhiser ◽  
Dora B. Madhura ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
In Vivo Efficacy

scholarly journals Furoxan derivatives demonstrated in vivo efficacy by reducing Mycobacterium tuberculosis to undetectable levels in a mouse model of infection

2020 ◽  
Vol 130 ◽  
pp. 110592
Author(s):  
P.C. de Souza ◽  
G.F.S. Fernandes ◽  
L.B. Marino ◽  
C.M. Ribeiro ◽  
P.B. da Silva ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Mouse Model ◽  
In Vivo Efficacy ◽  
Mouse Model Of Infection

Novel N-Linked Aminopiperidine-Based Gyrase Inhibitors with Improved hERG and in Vivo Efficacy against Mycobacterium tuberculosis

2014 ◽  
Vol 57 (11) ◽  
pp. 4889-4905 ◽  
Author(s):  
Shahul Hameed P ◽  
Vikas Patil ◽  
Suresh Solapure ◽  
Umender Sharma ◽  
Prashanti Madhavapeddi ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
In Vivo Efficacy ◽  
Gyrase Inhibitors
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