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

Peter B Madrid, Willma E Polgar, Lawrence Toll, Mary J Tanga

Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA. peter.madrid@sri.com

Bioorganic & medicinal chemistry letters 2007 Jun 1

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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.

Citation

Peter B Madrid, Willma E Polgar, Lawrence Toll, Mary J Tanga. Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors. Bioorganic & medicinal chemistry letters. 2007 Jun 1;17(11):3014-7