Mixture of trypaflavines (3,6-diamino-10-methylacridinium chloride and 3,6-diamino-3-methylacridinehydrochloride) and proflavine (3,6-diaminoacridine) hydrochloride
Acriflavine is an antimicrobial drug used to treat against sleeping sickness, urinary tract infections, and gonorrhea. Acriflavine is a potent inhibitor of SARS-CoV-2 papain-5 like protease (PLpro), which potently inhibits viral replication in vivo in mice and ex vivo in human airway epithelia. It is a mixture of trypaflavines (3,6-diamino-10-methylacridinium chloride and 3,6-diamino-3-methylacridinium chloride) and proflavine (3,6-diaminoacridine). Apparently commercial acriflavine mixtures contain the combination of differently methylated proflavines to optimally block the PLpro active site. Also, it potently inhibits replication of other betacoronaviruses.
Cell chemical biology, 29(5), 774-784 (2022-01-13)
The COVID-19 pandemic caused by SARS-CoV-2 has been socially and economically devastating. Despite an unprecedented research effort and available vaccines, effective therapeutics are still missing to limit severe disease and mortality. Using high-throughput screening, we identify acriflavine (ACF) as a
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