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1.
Eur J Med Chem ; 69: 591-600, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24095752

RESUMO

A series of 6-aryl-5-cyano thiouracil derivatives (2a-c to 11a-c) was synthesized from 6-aryl-4-hydrazino-2-thioxo-1,2-dihydropyrimidine-5-carbonitriles (1a-c). The products were characterized by analytical and spectral data (IR, (1)H NMR, (13)C NMR and mass spectra). All compounds were screened for their in-vitro antibacterial and antifungal activities. Compounds 7a, 7g and 9a-c showed pronounced antimicrobial activity than standards. Some of the newly synthesized compounds were evaluated for antioxidant activity. Compounds 1c, 5c and 8c displayed promising free radical scavenging activity and found to be more potent than standard, ascorbic acid (vitamin C).


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Tiouracila/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/química , Relação Dose-Resposta a Droga , Sequestradores de Radicais Livres/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Picratos/química , Relação Estrutura-Atividade , Tiouracila/síntese química , Tiouracila/química
3.
Drug Discov Ther ; 3(5): 200-7, 2009 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22495629

RESUMO

Expression profiling analysis offers great opportunities for the identification of novel molecular targets, drug discovery, development, and validation. The beauty of microarray analysis of gene expression is that it can be used to screen the expression of tens of thousands of genes in parallel and to identify appropriate molecular targets for therapeutic intervention. Toward identifying novel therapeutic options, natural products, notably from medicinal plants used in traditional Chinese medicine (TCM), have been thoroughly investigated. Increased knowledge of the molecular mechanisms of TCM-derived drugs could be achieved through application of modern molecular technologies including transcript profiling. In the present review, we introduce a brief introduction to the field of microarray technology and disclose its role in target identification and validation. Moreover, we provide examples for applications regarding molecular target discovery in medicinal plants derived TCM. This could be an attractive strategy for the development of novel and improved therapeutics.

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