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e-Article

Design, synthesis and evaluations of spiro‐fused benzoxaborin derivatives as novel boron‐containing compounds.
Document Type
Article
Source
Chemical Biology & Drug Design. May2019, Vol. 93 Issue 5, p657-665. 9p.
Subject
*DRUG design
*PHARMACOKINETICS
*BORON compounds
*IN vitro studies
*OXINDOLES
Language
ISSN
1747-0277
Abstract
Drug design using boron‐containing heterocycles has attracted a great deal of attention because these compounds are believed to possess high biological activity. However, information on the synthetic methodology and pharmacokinetic profiling of boron‐containing compounds is limited. In this study, we provide a new synthetic route for preparation of spiro‐fused benzoxaborin derivatives and investigate their in vitro pharmacokinetic properties. Our efforts led to the successful construction of a chemical library of spiro‐fused benzoxaborin derivatives with appropriate physicochemical and in vitro pharmacokinetic properties for oral drugs. These results indicate that the synthesized boron‐containing compounds are therefore eligible for classification in a novel chemical library. [ABSTRACT FROM AUTHOR]