Éthambutol | EPFL Graph Search

Ethambutol (EMB, E) is a medication primarily used to treat tuberculosis. It is usually given in combination with other tuberculosis medications, such as isoniazid, rifampicin and pyrazinamide. It may also be used to treat Mycobacterium avium complex, and Mycobacterium kansasii. It is taken by mouth. Common side effects include problems with vision, joint pain, nausea, headaches, and feeling tired. Other side effects include liver problems and allergic reactions. It is not recommended in people with optic neuritis, significant kidney problems, or under the age of five. Use during pregnancy or breastfeeding has not been found to cause harm. In the United States the FDA has raised concerns about eye issues in the baby if used during pregnancy. Ethambutol is believed to work by interfering with the bacteria's metabolism. Ethambutol was discovered in 1961. It is on the World Health Organization's List of Essential Medicines and is available as a generic medication. (S,S)-(+)-Ethambutol is powerful and selective antitubercular drug. It is a typical example of an old drug that was introduced for clinical use in its unichiral form. Ethambutol contains two constitutionally symmetrical chiral centers in its structure and exists in three stereoisomeric forms. An enantiomeric pair (S,S)- and (R,R)-ethmabutol, along with the achiral stereoisomer called meso-form. The (S,S)-(+)-enantiomer harbors the antitubercular activity. This enantiomer is 500 and 12 fold more potent than the (R,R)-ethmabutol and the meso-form respectively. On the other hand, all the three isomers are equipotent in terms of the major side-effect of the drug, optic neuritis. Toxicity is associated to both dose and duration of treatment. Hence the use of (S,S)-enantiomer greatly improved the risk/benefit balance. Ethambutol is used along with other medications to treat a number of infections including: tuberculosis, Mycobacterium avium complex, and Mycobacterium kansasii.

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Mycobacterium tuberculosis possesses a thick and highly hydrophobic cell wall principally composed of a mycolyl-arabinogalactan-peptidoglycan complex, which is critical for survival and virulence. DprE1 is a well-characterized component of decaprenyl-phosp ...

Amer Soc Microbiology2015

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Stewart Cole, Florence Pojer, Joao Pedro De Almeida Neres, Anirban Ghosh

We report the discovery of benzothiazoles, a novel anti-mycobacterial series, identified from a whole cell based screening campaign. Benzothiazoles exert their bactericidal activity against Mycobacterium tuberculosis (Mtb) through potent inhibition of deca ...

Elsevier2015