Synthesis and Myorelaxant Activity of Fused 1,4-Dihydropyridines on Isolated Rabbit Gastric Fundus

Safak C., GÜNDÜZ M. G., Ilhan S. O., ŞİMŞEK R., Isli F., Yildirim S., ...More

DRUG DEVELOPMENT RESEARCH, vol.73, no.6, pp.332-342, 2012 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 73 Issue: 6
  • Publication Date: 2012
  • Doi Number: 10.1002/ddr.21024
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.332-342
  • Keywords: condensed 1, 4-dihydropyridine, calcium channel modulator, myorelaxant activity, CALCIUM-CHANNEL ANTAGONIST, PHARMACOLOGICAL-ACTIVITIES, DERIVATIVES, MODULATORS, DESIGN, AGENTS
  • Hacettepe University Affiliated: Yes


Strategy, Management and Health Policy Preclinical Research In the present study, 25 novel condensed 1,4-dihydropyridine (DHP) derivatives bearing cyclopentane, cyclohexane, or tetrahydrothiopene ring with a bulky and lipophilic moiety (3-pyridylmethyl) in the ester group were synthesized via a modified Hantzsch reaction, and their calcium channel modulator activities were assayed on isolated rabbit gastric fundus smooth muscle strips. To evaluate the myorelaxant effects of the compounds, the maximum relaxant response (Emax) and pD 2 values were calculated. The results indicated that all compounds produced concentration-dependent relaxation and the introduction of five- or six-membered rings to the DHP nucleus and 3-pyridiylmethyl moiety to the ester group led to potent calcium antagonists.