Abstract
Conformational restriction constitutes a useful strategy of molecular modification for the design of new potential drug candidates. Herein we present the planning, antimicrobial evaluation, and establishment of structure–activity relationship (SAR) data for some isoxazole (
3a–k
,
8a–c
, and
9a–c
) and pyrazole (
5a–h
) derivatives. These derivatives were structurally designed by conformational restriction followed by bioisosteric exchange of previously described antimicrobial isoquinolines (
1a–c
). Some of these more conformationally restricted derivatives present improved properties as new antibacterial drug candidates.