Direct inhibitors of InhA are active against Mycobacterium tuberculosis
نویسندگان
چکیده
منابع مشابه
Indoleamides are active against drug-resistant Mycobacterium tuberculosis
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...
متن کاملDesigning of inhibitors against drug tolerant Mycobacterium tuberculosis (H37Rv)
BACKGROUND Mycobacterium tuberculosis (M.tb) is the causative agent of tuberculosis, killing ~1.7 million people annually. The remarkable capacity of this pathogen to escape the host immune system for decades and then to cause active tuberculosis disease, makes M.tb a successful pathogen. Currently available anti-mycobacterial therapy has poor compliance due to requirement of prolonged treatmen...
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in a combination of amino acids. It was subsequently found that a mixture of phenylalanine and cysteine promoted partial reversal of the inhibition, but that in the presence of a B vitamin supplement, the activity of the cysteine was less pronounced, whereas a mixture of phenylalanine and glutamic acid showed even greater activity. The activity of the vitamin supplement resided in its niacin an...
متن کامل2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains.
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...
متن کاملMefloquine and Its Enantiomers Are Active against Mycobacterium tuberculosis In Vitro and in Macrophages
Objective. Tuberculosis is a serious problem of public health. The increase on the number of clinical cases of tuberculosis infected with multidrug resistant (MDR) M. tuberculosis calls for the development of novel therapy. Design. We investigated the effect of mefloquine and two enantiomers, (+)erythro-mefloquine and (+)threo-mefloquine against M. tuberculosis strains in the environment resemb...
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ژورنال
عنوان ژورنال: Science Translational Medicine
سال: 2015
ISSN: 1946-6234,1946-6242
DOI: 10.1126/scitranslmed.3010597