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1. Synthesis of phenothiazine derivatives as potential inhibitors of phospholipase C

Author

Brufani M, Mc, Cesta, Filocamo L, Lappa S, Maurizio Marta, Pomponi M, Meroni C, and Pg, Pagella

Subjects
Blood Platelets, Structure-Activity Relationship, Phenothiazines, Type C Phospholipases, Humans, In Vitro Techniques
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.

Published
1992

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