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

PB Madrid, WE Polgar, L Toll, MJ Tanga

Index: Madrid, Peter B.; Polgar, Willma E.; Toll, Lawrence; Tanga, Mary J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 11 p. 3014 - 3017

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Citation Number: 55

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-HT1A, 5-HT2A, and 5-HT2C. The most active compounds showed MICs from 2 to 4μg/mL and had overall reduced binding to the ...