| Abstract
| - In an effort to develop potent new antituberculosis agents that would be effective against both drug-susceptibleand drug-resistant strains of Mycobacterium tuberculosis, we prepared a novel series of optically active6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles substituted at the 2-position with various phenoxymethyl groupsand a methyl group and investigated the in vitro and in vivo activity of these compounds. Several of thesederivatives showed potent in vitro and in vivo activity, and compound 19 (OPC-67683) in particular displayedexcellent in vitro activity against both drug-susceptible and drug-resistant strains of M. tuberculosis H37Rv(MIC = 0.006 μg/mL) and dose-dependent and significant in vivo efficacy at lower oral doses than rifampicinin mouse models infected with M. tuberculosis Kurono. The synthesis and structure−activity relationshipsof these new compounds are presented.
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