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Guanidinium compounds with sub-micromolar activities against Mycobacterium tuberculosis. Synthesis, characterization and biological evaluations

Abstract : Seven polycharged species, incorporating 1, 2, 3, 4 and 6 guanidine arms organized around a benzene core were synthesized and assayed as anti-mycobacterial agents against Mycobacterium tuberculosis. They display MIC values comprised between 25 and 12.5 mu M (close to ethambutol EMB) for the mono-and the hexa-substituted derivatives, and 0.8 mu M (close to isoniazid and streptomycin) for the tri-substituted derivative. The three bi- and the tetra-substituted analogs displayed MIC values of ca. 6.5-3.0 mu M. The latter were also evaluated against the isoniazid-resistant MYC5165 strain, resulting in highly interesting micromolar or sub-micromolar MIC, ca. 4-125 times more active than isoniazid. These preliminary results are attractive for the development of new anti-TB agents.
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https://hal.univ-lorraine.fr/hal-01495207
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Submitted on : Friday, March 24, 2017 - 4:22:54 PM
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Hugues Massimba-Dibama, Maxime Mourer, Patricia Constant, Mamadou Daffé, Jean-Bernard Regnouf-De-Vains. Guanidinium compounds with sub-micromolar activities against Mycobacterium tuberculosis. Synthesis, characterization and biological evaluations. Bioorganic and Medicinal Chemistry, Elsevier, 2015, 23 (17), pp.5410-5418. ⟨10.1016/j.bmc.2015.07.053⟩. ⟨hal-01495207⟩

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