Blank, Brian R. published the artcileAntimalarial Trioxolanes with Superior Drug-Like Properties and In Vivo Efficacy, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is antimalarials endoperoxides trioxolanes lead optimization stereoselective synthesis; antimalarials; endoperoxides; lead optimization; stereoselective synthesis; trioxolanes.
The emergence of artemisinin resistance, combined with certain suboptimal properties of ozonide agents arterolane and artefenomel, has necessitated the search for new drug candidates in the endoperoxide class. Our group has focused on trioxolane analogs with substitution patterns not previously explored. Here, we describe the enantioselective synthesis of analogs bearing a trans-3” carbamate side chain and find these to be superior, both in vitro and in vivo, to the previously reported amides. We identified multiple analogs that surpass the oral efficacy of arterolane in the Plasmodium berghei model while exhibiting drug-like properties (logD, solubility, metabolic stability) similar or superior to next-generation clin. candidates like E209 and OZ609. While the preclin. assessment of new analogs is still underway, current data suggest the potential of this chemotype as a likely source of future drug candidates from the endoperoxide class.
ACS Infectious Diseases published new progress about Antimalarials. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Name: tert-Butyl piperidin-4-ylcarbamate.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem