volume 28, issue 23-24, P3648-3651 2018
DOI: 10.1016/j.bmcl.2018.10.039
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Abstract: Urea carboxylic acids, products of aryl hydantoin hydrolysis, were recently identified as a new antischistosomal chemotype. We now describe a baseline structure-activity relationship (SAR) for this compound series. With one exception, analogs of lead urea carboxylic acid 2 were quite polar with LogD7.4 values ranging from −1.9 to 1.8, had high aqueous solubilities in the range of 25-100 μg/mL, and were metabolically stable. None of the compounds had measurable in vitro antischistosomal activity or cytotoxicit…

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