Synthesis and In vitro Efficacy of Tetracyclic Benzothiazepines Against Blood-Stage Plasmodium falciparum and Liver-Stage P. berghei .

Clare E Gutteridge,Brett W Sadowski, Stephen M Hughes, J Alan Friedlander, Alicia D Gaidry,Michael C Baxter, Matthew B Smith, Leighton G Rodrigo,Michael T O'Neil,Lucia Gerena,Patricia J Lee,Ramadas Sathunuru,Montip Gettayacamin

Medicinal chemistry (Shariqah (United Arab Emirates))（2023）

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摘要

The tetracyclic benzothiazepine described, which inhibits P. berghei infected hepatic cells with an IC of 106.4 nM, would appear to warrant further investigation. Optimization of ADME properties may be required since the most active analogs are probably excessively lipophilic.

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关键词

Benzothiazepines, benzoindenothiazepines, drug resistance, malaria, Plasmodium falciparum, structure-activity relationship

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