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Design, synthesis and evaluations of spiro‐fused benzoxaborin derivatives as novel boron‐containing compounds
Author(s) -
Natsutani Itaru,
Iwata Riyo,
Yamai Yusuke,
Ishida Kyoji,
Nagaoka Yasuo,
Sumiyoshi Takaaki
Publication year - 2019
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13496
Subject(s) - combinatorial chemistry , boron , pharmacokinetics , chemistry , in vitro , chemical synthesis , organic chemistry , pharmacology , biochemistry , medicine
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.