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1.
Drug Res (Stuttg) ; 67(5): 289-301, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-28268236

RESUMEN

The synthesized 4-(4-hydroxy benzyl)-2-amino-6-hydroxy pyrimidine-5-carboxamide was chosen to perform in silico modeling with identified drug target AGT, TNF, F2 and BCL2L1. The identified human proteins are vital in the pain management and also an important target for the study of wound healing activity. The enzymes were identified by using BioGRID, string database and network analysis through Cytoscape software. The wound healing activity was evaluated by excision wound model. The observed results revealed that, the pyrimidine nanoparticles showed significant wound healing activity compared to standard and synthesized compound. The detailed synthesis of nanoparticles formulation spectral analysis and pharmacological screening data's were reported. The revealed reports of synthesized analogues and formulated nanoparticles will generate a very good impact to the chemists and research scholars for further investigations in wound healing and pain management.


Asunto(s)
Nanopartículas/química , Pirimidinas/química , Pirimidinas/farmacología , Animales , Química Farmacéutica/métodos , Simulación por Computador , Humanos , Manejo del Dolor/métodos , Ratas , Cicatrización de Heridas/efectos de los fármacos
2.
Drug Discov Ther ; 10(4): 188-94, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27594295

RESUMEN

In this study, a series of novel scaffold-based 3-(((substituted phenyl)amino)methyl)-2-methylquinazolin-4(3H)-one compounds, 3a-3r, was synthesized, characterized, and screened for its in vitro activity against the H37Ra strain of Mycobacterium tuberculosis. A number of analogs were found to have highly potent anti-tuberculosis activity. Compound 3m in particular had potent activity equal to that of the standard anti-tuberculosis drug rifampicin. New leads can be generated with the model developed in this study and this model will be optimized with the eventual goal of preparing new anti-tuberculosis agents.


Asunto(s)
Antituberculosos/síntesis química , Diseño de Fármacos , Simulación del Acoplamiento Molecular , Mycobacterium tuberculosis/efectos de los fármacos , Quinazolinonas/síntesis química , Antituberculosos/farmacología , Simulación por Computador , Evaluación Preclínica de Medicamentos , Pruebas de Sensibilidad Microbiana , Quinazolinonas/farmacología , Rifampin/farmacología , Relación Estructura-Actividad
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