Outstanding effect of the conformational restriction of isoquinolines: Hints for the development of optimized antimicrobial agents

ÖZÇELİK B. , Sheikh J., Orhan İ. , Juneja H., Bennani B., Kerbal A., ...More

Research on Chemical Intermediates, vol.39, no.7, pp.2955-2962, 2013 (Journal Indexed in SCI Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 39 Issue: 7
  • Publication Date: 2013
  • Doi Number: 10.1007/s11164-012-0808-2
  • Title of Journal : Research on Chemical Intermediates
  • Page Numbers: pp.2955-2962


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. © 2012 Springer Science+Business Media B.V.