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1.
Artículo en Inglés | MEDLINE | ID: mdl-35261779

RESUMEN

Hearing aids help overcome the challenges associated with hearing loss, and thus greatly benefit and improve the lives of those living with hearing-impairment. Unfortunately, there is a lack of adoption of hearing aids among those that can benefit from hearing aids. Hearing researchers and audiologists are trying to address this problem through their research. However, the current proprietary hearing aid market makes it difficult for academic researchers to translate their findings into commercial use. In order to abridge this gap and accelerate research in hearing health care, we present the design and implementation of the Open Speech Platform (OSP), which consists of a co-design of open-source hardware and software. The hardware meets the industry standards and enables researchers to conduct experiments in the field. The software is designed with a systematic and modular approach to standardize algorithm implementation and simplify user interface development. We evaluate the performance of OSP regarding both its hardware and software, as well as demonstrate its usefulness via a self-fitting study involving human participants.

2.
Biochem J ; 406(3): 407-14, 2007 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-17581113

RESUMEN

The release of GA (mitochondrial glutaminase) from neurons following acute ischaemia or during chronic neurodegenerative diseases may contribute to the propagation of glutamate excitotoxicity. Thus an inhibitor that selectively inactivates the released GA may limit the accumulation of excess glutamate and minimize the loss of neurological function that accompanies brain injury. The present study examines the mechanism of inactivation of rat KGA (kidney GA isoform) by the small-molecule inhibitor BPTES [bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide]. BPTES is a potent inhibitor of KGA, but not of the liver GA isoform, glutamate dehydrogenase or gamma-glutamyl transpeptidase. Kinetic studies indicate that, with respect to glutamine, BPTES has a K(i) of approx. 3 microM. Moreover, these studies suggest that BPTES inhibits the allosteric activation caused by phosphate binding and promotes the formation of an inactive complex. Gel-filtration chromatography and sedimentation-velocity analysis were used to examine the effect of BPTES on the phosphate-dependent oligomerization of KGA. This established that BPTES prevents the formation of large phosphate-induced oligomers and instead promotes the formation of a single oligomeric species with distinct physical properties. Sedimentation-equilibrium studies determined that the oligomer produced by BPTES is a stable tetramer. Taken together, the present work indicates that BPTES is a unique and potent inhibitor of rat KGA and elucidates a novel mechanism of inactivation.


Asunto(s)
Inhibidores Enzimáticos/farmacología , Glutaminasa/antagonistas & inhibidores , Riñón/enzimología , Sulfuros/farmacología , Tiadiazoles/farmacología , Animales , Cromatografía en Gel , Fraccionamiento de Campo-Flujo , Glutaminasa/metabolismo , Riñón/crecimiento & desarrollo , Cinética , Ratas , Ratas Sprague-Dawley , Ultracentrifugación
3.
Org Lett ; 7(12): 2429-31, 2005 Jun 09.
Artículo en Inglés | MEDLINE | ID: mdl-15932215

RESUMEN

[reaction: see text] A mild, efficient, and high-yielding method for the synthesis of N,N'-diaryl cyanoguanidines from their corresponding thioureas under microwave-assisted conditions is described. A series of cyanoguanidines were synthesized containing both electron-donating and electron-withdrawing substituents. The reactions were facilitated by the use of polar solvents along with moderate temperatures.


Asunto(s)
Guanidinas/síntesis química , Microondas , Catálisis , Estructura Molecular , Sulfuros/síntesis química , Temperatura
4.
J Org Chem ; 67(21): 7553-6, 2002 Oct 18.
Artículo en Inglés | MEDLINE | ID: mdl-12375997

RESUMEN

A direct synthetic approach to guanidine compounds is reported here using di(imidazole-1-yl)methanimine and di(imidazole-1-yl)cyanomethanimine as guanylating reagents.


Asunto(s)
Guanidinas/síntesis química , Guanidinas/química , Imidazoles , Indicadores y Reactivos , Espectroscopía de Resonancia Magnética , Metilaminas , Modelos Moleculares , Estructura Molecular , Relación Estructura-Actividad
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