molecules of the month

compound 7

oral 20S proteasome inhibitor

efficacy in stage II mouse model of HAT

3 million cmpd HTS and SBDD

J. Med. Chem.

Novartis Institutes for Biomedical Research, Emeryville, CA

compound 7 chemical structure oral 20S proteasome inhibitor - Novartis Institutes for Biomedical Research, Emeryville, CA
5 mins read

Context. “Compound 7” (NIBR) is an oral Trypanosoma brucei 20S proteasome inhibitor being developed for Human African Trypanosomiasis (HAT). African sleeping sickness, or HAT, is caused by a parasite in the genus Trypanosoma.  The parasite is spread by the Tsetse fly, and the lifecycle of the parasite involves a phase in the blood of the host, followed by a devastating phase in the brain of the host. Melarsoprol, the prodrug of arsenic-containing melarsen oxide, was the first treatment for second-phase HAT since 1942 but was highly neurotoxic and brought widespread resistance in the 1990s. In 2009, the introduction of NECT, nifurtimox, an antiparasitic for Chagas disease caused by T. cruzi, combined with IV administration of eflornithine, an irreversible inhibitor of…

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