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ChemMedChem ; 8(2): 313-21, 2013 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-23307663

RESUMO

With the aim of fuelling open-source, translational, early-stage drug discovery activities, the results of the recently completed antimycobacterial phenotypic screening campaign against Mycobacterium bovis BCG with hit confirmation in M. tuberculosis H37Rv were made publicly accessible. A set of 177 potent non-cytotoxic H37Rv hits was identified and will be made available to maximize the potential impact of the compounds toward a chemical genetics/proteomics exercise, while at the same time providing a plethora of potential starting points for new synthetic lead-generation activities. Two additional drug-discovery-relevant datasets are included: a) a drug-like property analysis reflecting the latest lead-like guidelines and b) an early lead-generation package of the most promising hits within the clusters identified.


Assuntos
Antituberculosos/química , Antituberculosos/farmacologia , Descoberta de Drogas/métodos , Mycobacterium bovis/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Bibliotecas de Moléculas Pequenas/química , Bibliotecas de Moléculas Pequenas/farmacologia , Bases de Dados de Produtos Farmacêuticos , Células Hep G2 , Ensaios de Triagem em Larga Escala , Humanos , Testes de Sensibilidade Microbiana , Tuberculose/tratamento farmacológico
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