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

Creative Commons License

Özçelik B., Sheikh J., Orhan İ., Juneja H., Bennani B., Kerbal A., ...Daha Fazla

Research on Chemical Intermediates, cilt.39, sa.7, ss.2955-2962, 2013 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 39 Sayı: 7
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1007/s11164-012-0808-2
  • Dergi Adı: Research on Chemical Intermediates
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED)
  • Sayfa Sayıları: ss.2955-2962
  • Gazi Üniversitesi Adresli: Evet

Özet

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.