Condensed 1,4-dihydropyridines with various esters and their calcium channel antagonist activities

Eur J Med Chem. 2009 May;44(5):2052-8. doi: 10.1016/j.ejmech.2008.10.008. Epub 2008 Nov 1.

Abstract

New alkyl 2,6,6-(2,7,7)-trimethyl-4-(2-fluoro-3-chloro-5-trifluoromethylphenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates and 9-(3-chloro-2-fluoro-5-trifluoromethylphenyl)-6,6(7,7)-dimethyl-6,7-dihydrofuro[3,4-b]quinoline-1,8-diones have been synthesised and their calcium antagonistic activities on isolated rabbit sigmoid colon have been investigated and compared with Nifedipine. The investigation examined the influence of ester groups in the 3-position of the HHQ ring and the 2-methoxyethyl analogs were found to be the most active derivatives.

MeSH terms

  • Animals
  • Calcium Channel Blockers / chemistry*
  • Colon / drug effects
  • Dihydropyridines / chemistry*
  • Dihydropyridines / pharmacology
  • Esters
  • In Vitro Techniques
  • Rabbits
  • Structure-Activity Relationship

Substances

  • Calcium Channel Blockers
  • Dihydropyridines
  • Esters