Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors

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• 作者：Peter B. Madrid ; Willma E. Polgar ; Lawrence Toll ; Mary J. Tanga
• 关键词：Tuberculosis ; Antitubercular agents ; Phenothiazines ; NADH dehydrogenase II
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 June 2007
• 卷：17
• 期：11
• 页码：3014-3017
• 文件大小：161 K

摘要

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-HT_1A, 5-HT_2A, and 5-HT_2C. 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.