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  • 标题:Synthesis and photodegradation studies of analogues of muscle relaxant 1,4-dihydropyridine compounds
  • 本地全文:下载
  • 作者:MIYASE GÖZDE GÜNDÜZ ; GAETANO RAGNO ; RAHIME ŞIMŞEK
  • 期刊名称:Acta Pharmaceutica
  • 电子版ISSN:1846-9558
  • 出版年度:2017
  • 卷号:67
  • 期号:3
  • 页码:341-355
  • DOI:10.1515/acph-2017-0026
  • 语种:English
  • 出版社:Sciendo
  • 摘要:This paper describes the synthesis of 1,4-dihydropyridine compounds (DHPs) endowed with good muscle relaxant activity and stability to light.Six new condensed DHPs were synthesized by the microwave irradiation method.A long-chain ester moiety [2-(methacryloyloxy)ethyl] and various substituents on the phenyl ring were demonstrated to aff ect the muscle relaxant activity occurring in isolated rabbit gastric fundus smooth muscle strips.Forced photodegradation conditions were applied to the molecules according to the ICH rules.The degradation profi le of the drugs was monitored by spectrophotometry coupled with the multivariate curve resolution technique.Formation of the oxidized pyridine derivative was observed for all the studied DHPs,except for one compound,which showed very fast degradation and formation of a second photoproduct.Pharmacological tests on the molecules showed a good muscle relaxing eff ect,with a mechanism similar to that of nifedipine,however,proving to be more stable to light.
  • 关键词:1;4-dihydropyridine compounds;muscle relaxant;drug design;structure activity relationship;photostability;MCR analysis
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