1,5-Benzothiazepine, a versatile pharmacophore: a review

Eur J Med Chem. 2008 Nov;43(11):2279-90. doi: 10.1016/j.ejmech.2008.05.035. Epub 2008 Jun 6.


1,5-Benzothiazepine and 1,5-benzodiazipine are the two main seven-membered heterocyclic ring systems reported for their cardiac and psychotherapeutic activities. Successful introduction of diltiazem and clentiazem for angina pectoris, hypertension, arrhythmias and other related cardiac disorders proved potential of 1,5-benzothiazepine moiety. Subsequently 1,5-benzodiazepines were highlighted as important biologically active scaffolds. Also, discovery of thiazesim and quetiapine fumarate as psychotropic agents attracted much attention worldwide. The current review article focuses on pharmacological profile associated with 1,5-benzodiazepines. This article mainly covers structural modifications done for various targets along with the brief description of the targets.

Publication types

  • Review

MeSH terms

  • Animals
  • Benzodiazepines / chemistry*
  • Benzodiazepines / pharmacology
  • Calcium Channel Blockers / chemistry
  • Calmodulin / antagonists & inhibitors
  • Calmodulin / metabolism
  • Central Nervous System / drug effects
  • Central Nervous System / metabolism
  • Humans
  • Platelet Aggregation / drug effects


  • Calcium Channel Blockers
  • Calmodulin
  • Benzodiazepines