Exploring selectivity requirements for COX-2 versus COX-1 binding of 3,4-diaryloxazolones using E-state index

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3753-7. doi: 10.1016/j.bmcl.2003.07.002.

Abstract

Considering the importance of developing selective COX-2 inhibitors, the present paper explores selectivity requirements for COX-2 versus COX-1 binding of 3,4-diaryloxazolones using electrotopological state (E-state) index. The study also shows the utility of E-state index in developing statistically acceptable model having direct physicochemical significance: electron density distribution of different atoms of the oxazolone ring and attached two phenyl rings are important for the selective binding with COX-2 over COX-1. Moreover, the use of indicator variable shows that presence of ortho R(1) substituent (except fluoro) on the N(3)-phenyl ring decreases COX-2 selectivity. Further, an amino substituent at R(2) position (i.e., sulfonamide compound) is favorable for increasing COX-2 selectivity when the R(3) position is unsubstituted.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemical Phenomena
  • Chemistry, Physical
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / pharmacology*
  • Isoenzymes / chemistry
  • Isoenzymes / drug effects*
  • Oxazolone / analogs & derivatives*
  • Oxazolone / chemical synthesis*
  • Oxazolone / pharmacology*
  • Prostaglandin-Endoperoxide Synthases / chemistry
  • Prostaglandin-Endoperoxide Synthases / drug effects*
  • Structure-Activity Relationship

Substances

  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Oxazolone
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Prostaglandin-Endoperoxide Synthases