Title : Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro.

Pub. Date : 2021 Aug 12

PMID : 34413963






1 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 Among 46 analogues tested, compounds 21, 30, and 33 displayed high activities against asexual blood stage parasites (PfNF54 IC50 = 0.025-0.043 muM), whereas amide compound 46 additionally showed activity against late-stage gametocytes (stage IV/V; PfLG IC50 = 0.6 +- 0.1 muM) and 860-fold higher selectivity over hERG (46, SI = 43) compared to AST. Amides ETS transcription factor ERG Homo sapiens