کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1366539 | 981595 | 2007 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors](/preview/png/1366539.png)
Analogs of the psychotropic phenothiazines were synthesized and examined as antitubercular agents against Mycobacterium tuberculosis H37Rv. The compounds were subsequently counter-screened for binding to the dopaminergic-receptor subtypes D1, D2, D3 and the serotonergic-receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2C. The most active compounds showed MICs from 2 to 4 μg/mL and had overall reduced binding to the dopamine and serotonin receptors compared to chlorpromazine and trifluoperazine.
A series of phenothiazines were synthesized and evaluated for activity against Mycobacterium tuberculosis. The compounds were subsequently counter-screened for binding to dopamine and serotonin receptors to determine the in vitro selectivity of the compounds for antitubercular activity over psychotropic effects.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 11, 1 June 2007, Pages 3014–3017