학술논문
Outstanding effect of the conformational restriction of isoquinolines: hints for the development of optimized antimicrobial agents.
Document Type
Article
Author
Source
Subject
*CONFORMATIONAL analysis
*ISOQUINOLINE
*ANTI-infective agents
*BIOISOSTERES
*ISOXAZOLES
*PYRAZOLES
*
*
*
*
*
Language
ISSN
0922-6168
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. [ABSTRACT FROM AUTHOR]