1401710-57-3Relevant academic research and scientific papers
Synthesis and pharmacological investigation of new N-hydroxyalkyl-2- aminophenothiazines exhibiting marked MDR inhibitory effect
Takacs, Daniella,Egyed, Orsolya,Drahos, Laszlo,Szabo, Pal,Jemnitz, Katalin,Szabo, Monika,Veres, Zsuzsa,Visy, Julia,Molnar, Jozsef,Riedl, Zsuzsanna,Hajos, Gyoergy
, p. 3760 - 3779 (2013/07/25)
Novel N-hydroxyalkyl-2-aminophenothiazines implying a tetrazole moiety at the alkyl chain have been synthesized by hydroboration-oxidation of dienes followed by Buchwald-Hartwig cross-coupling reaction. Also, some sulfoxide and sulfone derivatives have been prepared by selective oxidations. MDR inhibition studies on rat hepatocyte cell culture revealed that some derivatives exhibit marked biological efficacy exceeding that of the standard verapamil (e.g., 3h, 4h, 16). Selected derivatives were subjected to chemical resolution to provide both enantiomers which were shown of similar activity on P-gp interaction measurements. The new compounds exhibited no toxicity.
A new synthetic approach to phenothiazine-2-amines
Takács, Daniella,Egyed, Orsolya,Drahos, László,Riedl, Zsuzsanna,Hajós, Gy?rgy
supporting information, p. 5585 - 5588 (2012/10/29)
Elaboration of a Buchwald-Hartwig protocol for the introduction of amino functions to position 2 of the phenothiazine ring system has opened a new access to various N-alkyl and N-dienyl phenothiazines bearing secondary amines, tertiary amines, and amide moieties. Hydrolysis of the amido derivatives gave unsubstituted phenothiazine-2-amines. This protocol provides an easy access to phenothiazine-2-amines starting from the commercially available starting compounds.
