Spirooxindoles as novel 3D-fragment scaffolds: Synthesis and screening against CYP121 from $\textit{M. tuberculosis}$

Holly J Davis, Madeline Kavanagh, Tudor Balan, Christopher Abell & Anthony Coyne
The search for new scaffolds to complement current HTS and fragment libraries is an active area of research. The development of novel strategies to synthesise compounds with 3D character in order to expand the diversity of a fragment library was explored. A range of substituted bicyclo[2,2,1]spirooxindoles were synthesised using a Diels–Alder [4+2] cycloaddition reaction. Both diastereoisomers were isolated from the reactions and these 3D fragment scaffolds were screened against the cytochrome P450 enzyme CYP121 from...

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