title: Synthesis of phenothiazine derivatives as potential inhibitors of phospholipase C.
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.
authors.affiliation: Dipartimento di Scienze Biochimiche A. Rossi Fanelli, Università La Sapienza, Roma, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Brufani
authors.forename: M C
authors.initials: MC
authors.lastname: Cesta
authors.forename: L
authors.initials: L
authors.lastname: Filocamo
authors.forename: S
authors.initials: S
authors.lastname: Lappa
authors.forename: M
authors.initials: M
authors.lastname: Marta
authors.forename: M
authors.initials: M
authors.lastname: Pomponi
authors.forename: C
authors.initials: C
authors.lastname: Meroni
authors.forename: P G
authors.initials: PG
authors.lastname: Pagella
mesh_terms: 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*
chemical_list: D010640:Phenothiazines; D010738:Type C Phospholipases