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

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Madrid PB, Polgar WE, Toll L, Tanga MJ

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

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3014-7. Epub 2007 Mar 24.

PubMed ID

17407813 [ View in PubMed

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Abstract

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 microg/mL and had overall reduced binding to the dopamine and serotonin receptors compared to chlorpromazine and trifluoperazine.

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Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Trifluoperazine	Neuron-specific vesicular protein calcyon	Protein	Humans	Yes	Antagonist	Details