Synthesis and calcium modulatory activity of 3-alkyloxycarbonyl-4-(disubstituted)aryl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives


ŞİMŞEK R. , Ozturk G. S. , Vural I. M. , GÜNDÜZ M. G. , Sarioglu Y., Safak C.

ARCHIV DER PHARMAZIE, cilt.341, sa.1, ss.55-60, 2008 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 341 Konu: 1
  • Basım Tarihi: 2008
  • Doi Numarası: 10.1002/ardp.200700087
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Sayfa Sayıları: ss.55-60

Özet

In this study, twelve hexahydroquinoline derivatives which are condensed analogs of the 1,4-DHP molecule were synthesized and evaluated for their calcium-antagonistic activity. The results indicated that all compounds and nifedipine produced concentration-dependent relaxation in rabbit gastric fundus smooth muscle strips. The relaxant effects of the compounds on the tissues were expressed as percentage of the precontraction using Ca2+. The maximum response (E-max) and pD(2) values (the negative logarithm of the concentration for the half-maximal response (EC50)) were calculated. It is generally believed that introduction of a second electron-withdrawing substituent into the phenyl ring increases the mentioned activity. Methyl-2,7,7-trimethyl-4-(2-nitro-5-chlorophenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate 2a has been found to be the most active compound in this serie.