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Probing the B- & C-rings of the antimalarial tetrahydro-β-carboline MMV008138 for steric and conformational constraints

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 t...

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Dettagli Bibliografici
Pubblicato in:Bioorg Med Chem Lett
Autori principali: Ding, Sha, Ghavami, Maryam, Butler, Joshua H., Merino, Emilio F., Slebodnick, Carla, Cassera, Maria B., Carlier, Paul R.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2020
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC7686247/
https://ncbi.nlm.nih.gov/pubmed/32898696
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2020.127520
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