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conformational constraints

Not Open Access | Probing the B- & C-rings of the antimalarial tetrahydro-β-carboline MMV008138 for steric and conformational constraints

September 10, 2020 - 08:33 -- NOT Open Access
Author(s): 
Ding S, Ghavami M, Butler JH, Merino EF, Slebodnick C, Cassera MB, Carlier PR
Reference: 
Bioorg Med Chem Lett. 2020 Sep 5:127520

The antimalarial candidate MMV008138 (1a) is of particular interest because its target enzyme (IspD) is absent in human. To achieve higher potency, and to probe for steric demand, a series of analogs of 1a were prepared that featured methyl-substitution of the B- and C-rings, as well as ring-chain transformations.

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