Synthesis of phenothiazine derivatives as potential inhibitors of phospholipase C.
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.
Brufani
M
M
Dipartimento di Scienze Biochimiche A. Rossi Fanelli, Università La Sapienza, Roma, Italy.
Cesta
M C
MC
Filocamo
L
L
Lappa
S
S
Marta
M
M
Pomponi
M
M
Meroni
C
C
Pagella
P G
PG
D001792:Blood Platelets / Q000201:enzymology; D006801:Humans; D066298:In Vitro Techniques; D010640:Phenothiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D010738:Type C Phospholipases / Q000037:antagonists & inhibitors*
D010640:Phenothiazines; D010738:Type C Phospholipases