Structure–Activity Relationship of Antischistosomal Aryl Hydantoin (AR102)

As exemplified by Ro 13–3978 (<b>1</b>), aryl hydantoins were identified in the early 1980s as a promising antischistosomal chemotype. We now describe the structure–activity relationship (SAR) of this compound series, which led to the discovery of the drug development candidate AR102 (&l...

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Bibliographic Details
Main Author:	Derek A. Leas (4012631) (author)
Other Authors:	Cécile Häberli (6184631) (author), Karen L. White (1304598) (author), David M. Shackleford (1294671) (author), Jeremy O. Jones (773341) (author), Michael Campbell (562588) (author), Jianbo Wu (165270) (author), Deepender Kaushik (18550810) (author), Yuxiang Dong (1377870) (author), Alexander I. Wallick (8600538) (author), Susan A. Charman (1294689) (author), Jennifer Keiser (39606) (author), Paul H. Davis (373403) (author), Jonathan L. Vennerstrom (503780) (author)
Published:	2025
Subjects:	Biophysics Biochemistry Medicine Cell Biology Pharmacology Plant Biology Computational Biology Chemical Sciences not elsewhere classified vitro adme profiles two key advances aqueous kinetic solubilities abolish antiandrogenic effects >- dimethyl substructure 2 – 3 promising antischistosomal chemotype aryl trifluoromethyl substituent antischistosomal aryl hydantoin max </ sub 4 </ sub 1 </ b aryl hydantoins antischistosomal activity gem </ c </ >< sub slow phase one exception measured logd hydrogen atoms highest exposures fluorine atoms early 1980s direct correlation difluoropropyl substituents compound series 100 μg
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Structure–Activity Relationship of Antischistosomal Aryl Hydantoin (AR102)

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