3-(Phenethylamino)demethyl(oxy)aaptamine as an anti-dormant mycobacterial substance: Isolation, evaluation and total synthesis
2020; Elsevier BV; Volume: 61; Issue: 22 Linguagem: Inglês
10.1016/j.tetlet.2020.151924
ISSN1873-3581
AutoresYuji Sumii, Naoyuki Kotoku, Chisu Han, Kentaro Kamiya, Andi Setiawan, Catherine Vilchèze, William R. Jacobs, Masayoshi Arai,
Tópico(s)Mycobacterium research and diagnosis
Resumo3-(Phenethylamino)demethyl(oxy)aaptamine (1) was re-discovered from the marine sponge of Aaptos sp. as an anti-dormant mycobacterial substance through the bioassay-guided separation. Compound 1 showed potent anti-microbial activity against Mycobacterium bovis BCG with a minimum inhibitory concentration of 0.75 µg/mL under both aerobic conditions and hypoxic conditions inducing dormant state. Compound 1 was also effective against pathogenic M. tuberculosis strains including clinical multidrug-resistant strains. Furthermore, the successful total syntheses of 1 and its analog 3-aminodemethyl(oxy)aaptamine (2) afford sufficient quantities for further biological studies.
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