Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis
نویسندگان
چکیده
منابع مشابه
Thioridazine: an old neuroleptic effective against totally drug resistant tuberculosis.
Globally, tuberculosis infections continue to increase their resistance to antibiotics. Multidrug resistant tuberculosis infections (MDR TB) have progressed to extensively drug resistance status (XDR TB) and the latter have evolved in some parts of the world to totally drug resistant (TDR TB) infections. MDR TB is difficult to treat successfully, and when therapy is ineffective, a single case c...
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Responsible for nearly two million deaths each year, the infectious disease tuberculosis remains a serious global health challenge. The emergence of multidrug- and extensively drug-resistant strains of Mycobacterium tuberculosis confounds control efforts, and new drugs with novel molecular targets are desperately needed. Here we describe lead compounds, the indoleamides, with potent activity ag...
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2-(Quinolin-4-yloxy)acetamides have been described as potent in vitro inhibitors of Mycobacterium tuberculosis growth. Herein, additional chemical modifications of lead compounds were carried out, yielding highly potent antitubercular agents with minimum inhibitory concentration (MIC) values as low as 0.05 μM. Further, the synthesized compounds were active against drug-resistant strains and wer...
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ژورنال
عنوان ژورنال: European Journal of Medicinal Chemistry
سال: 2017
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2016.12.042