Abstract
We designed and synthesized AHI4 that has an axial hydroxyl group instead of geminal methyl groups at C-6′ of AHI1, previously reported as a lead compound for the development of non-azole inhibitors of ABA 8′-hydroxylase. (+)-AHI4 competitively inhibited 8′-hydroxylation of ABA by recombinant CYP707A3. The K I value was found to be 0.14 μM, 10-fold less than that of (+)-AHI1, suggesting that enzyme affinity increased by a factor of 10 due to substitution of the hydroxyl group by the geminal methyls at C-6′. This finding should assist in the design of more effective, non-azole ABA 8′-hydroxylase inhibitors.
Published Version
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