Sumii, Yuji and Kotoku, Naoyuki and Han, Chisu and Kamiya, Kentaro and Setiawan, Andi and Vilchèze, Catherine and Jacob Jr, William R and Arai, Masayoshi 3-(Phenethylamino)demethyl(oxy)aaptamine as an anti-dormant mycobacterial substance: Isolation, evaluation and total synthesis. Tetrahedron letter.

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3-(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.

Item Type: Other
Subjects: Q Science > Q Science (General)
Depositing User: Prof Andi Setiawan
Date Deposited: 18 Feb 2022 01:19
Last Modified: 18 Feb 2022 01:19

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