Synthesis of phenothiazine derivatives as potential inhibitors of phospholipase C

Farmaco. 1992 May;47(5):585-97.

Abstract

In order to study the structure-activity relationships of phenothiazine derivatives inhibiting phosphatidylinositol-specific phospholipase C (PI-PLC), the synthesis of some phenothiazine amide, amine and ester derivatives was performed mainly by reacting 10H-phenothiazine-10-propanoyl chloride with some amines and alcohols; the resulting amides were reduced with borane to yield the corresponding amines. Starting from 2-chloro and 2-trifluoromethyl-10H-phenothiazine-10-propanoyl chloride two amides were synthesized. The inhibiting activity on PI-PLC from human platelets is reported.

MeSH terms

  • Blood Platelets / enzymology
  • Humans
  • In Vitro Techniques
  • Phenothiazines / chemical synthesis*
  • Phenothiazines / pharmacology
  • Structure-Activity Relationship
  • Type C Phospholipases / antagonists & inhibitors*

Substances

  • Phenothiazines
  • Type C Phospholipases